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Journal articles on the topic 'Pyrimidine synthesis'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Verma, Vishal, Chandra Prakash Joshi, Alka Agarwal, Sakshi Soni, and Udichi Kataria. "A Review on Pharmacological Aspects of Pyrimidine Derivatives." Journal of Drug Delivery and Therapeutics 10, no. 5 (2020): 358–61. http://dx.doi.org/10.22270/jddt.v10i5.4295.

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Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogens at positions 1 and 3 in the ring. Pyrimidines are typically synthesized by the “Principal Synthesis” involving cyclization of beta-dicarbonyl compounds with N-C-N compounds. Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidiones, and guanidines to give 2-aminopyrimidines are typical. Pyrimidines can be prepared via the biginelli reaction. Many other methods

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2

Hossain, M. I., and M. M. H. Bhuiyan. "Synthesis and Antimicrobial Activities of Some New Thieno and Furopyrimidine Derivatives." Journal of Scientific Research 1, no. 2 (2009): 317–25. http://dx.doi.org/10.3329/jsr.v1i2.2299.

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Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6 dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitril

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3

Borrell, José I., Jordi Teixidó, Blanca Martínez-Teipel, et al. "An Unequivocal Synthesis of 4-Amino-1,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-2,7-diones and 2-Amino-3,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-4,7-diones." Collection of Czechoslovak Chemical Communications 61, no. 6 (1996): 901–9. http://dx.doi.org/10.1135/cccc19960901.

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An unequivocal set of procedures for the synthesis of 4-amino-1,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-2,7-diones (7) and 2-amino-3,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-4,7-diones (8), in a maximum of four steps from an α,β-unsaturated ester 1, is reported. Thus, the acid hydrolysis of the 2,4-diaminopyrido[2,3-d]pyrimidines 3 yields the 4-amino-2-oxopyrido[2,3-d]pyrimidines 7 while the cyclization of the Michael adducts 9 (formed by reaction of 1 and methyl cyanoacetate) with guanidine affords the corresponding 2-amino-4-oxopyrido[2,3-d]pyrimidines 8. Both isomers were also obtained by hy

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4

Sirakanyan, Spinelli, Geronikaki, et al. "Synthesis, Antitumor Activity, and Docking Analysis of New Pyrido[3’,2’:4,5]furo(thieno)[3,2-d]pyrimidin-8-amines." Molecules 24, no. 21 (2019): 3952. http://dx.doi.org/10.3390/molecules24213952.

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Continuing our research in the field of new heterocyclic compounds, herein we report on the synthesis and antitumor activity of new amino derivatives of pyrido[3’,2’:4,5](furo)thieno[3,2-d]pyrimidines as well as of two new heterocyclic systems: furo[2–e]imidazo[1,2-c]pyrimidine and furo[2,3-e]pyrimido[1,2-c]pyrimidine. Thus, by refluxing the 8-chloro derivatives of pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidines with various amines, the relevant pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidin-8-amines were obtained. Further, the cyclization of some amines under the action of phosphorus oxychlori

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5

Azam, Mohammed Afzal, Loganathan Dharanya, Charu Chandrakant Mehta, and Sumit Sachdeva. "Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system." Acta Pharmaceutica 63, no. 1 (2013): 19–30. http://dx.doi.org/10.2478/acph-2013-0001.

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In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeru

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6

Agarkov, Artem S., Dilyara O. Mingazhetdinova, Anna A. Nefedova, et al. "Synthesis and Structure of 6-Acetyl-2-Arylhydrazone Derivatives of Thiazolo[3,2-a]Pyrimidine." Organics 4, no. 3 (2023): 438–46. http://dx.doi.org/10.3390/org4030031.

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Triazolo[4,3-a]pyrimidine is one of the promising structural fragments for the development of drugs, including anticancer drugs. This work is devoted to the synthesis of a number of new 2-arylhydrazone derivatives of thiazolo[3,2-a]pyrimidine, which are synthetic precursors for triazolo[4,3-a]pyrimidines. The crystal structure of 6-acetyl-7-methyl-5-phenyl-2-(2-phenylhydrazineylidene)-5H-thiazolo[3,2-a]pyrimidin-3(2H)-one was established by SCXRD. In the reduction reaction of the compound, the following system was used: vanadium(V) oxide, and sodium borohydride in ethanol at room temperature,

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7

Ho, Yuh-Wen, and Maw Cherng Suen. "Thioxopyrimidine in Heterocyclic Synthesis I: Synthesis of Some Novel 6-(Heteroatom-substituted)-(thio)pyrimidine Derivatives." Journal of Chemistry 2013 (2013): 1–15. http://dx.doi.org/10.1155/2013/765243.

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A series of novel N-cycloalkanes, morpholine, piperazines, pyrazole, pyrimidine, benzimidazolo[1,2-a]pyrimidine, 1,2,3,4-tetrazolo[1,5-a]pyrimidine, azopyrazolo[1,5- a]pyrimidine, pyrimido[4', 5':3,4]pyrazolo[1,5-a]pyrimidines and pyridine derivatives incorporating a 5-cyano-4-methyl-2-phenyl-(thio)pyrimidine moiety were obtained by the intramolecular cyclization of 6-methylthio-pyrimidine, 6-(benzoylmethyl)thio- pyrimidine and 2-[(5-cyano-4-methyl-2-phenylpyrimidin-6-yl)thio]-3-dimethyl- amino-1-phenyl-prop-2-en-1-one with appropriate amines and enaminone compounds, respectively. The structur

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8

Mosaad, Sayed Mohamed, Mohamed Awad Samir, Abdallah Abd El-tawab Neama, and Mohamed Ahmed Naglaa. "An overview on synthesis and biological activity of pyrimidines." World Journal of Advanced Research and Reviews 15, no. 1 (2022): 272–96. https://doi.org/10.5281/zenodo.7743045.

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Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 of the six membered ring show wide range of biological activities. Numerous methods for the synthesis of pyrimidine and their diverse reactions offer enormous scope in the field of medicinal chemistry. Pyrimidine possesses wide spectrum of biological activities including antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer, and anti-HIV activity. The present review attempts to give brief information about the synthesis and various biological ac

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9

Mohammed, F. K., and M. G. Badrey. "Synthesis of Pyrimidines and Heteroannulated Pyrimidine Ring Systems." Journal of the Korean Chemical Society 55, no. 2 (2011): 218–29. http://dx.doi.org/10.5012/jkcs.2011.55.2.218.

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10

Venugopala, Katharigatta N., and Vinuta Kamat. "Pyrimidines: A New Versatile Molecule in the Drug Development Field, Scope, and Future Aspects." Pharmaceuticals 17, no. 10 (2024): 1258. http://dx.doi.org/10.3390/ph17101258.

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Pyrimidine is a moiety that occurs in living organisms and has a variety of significant biological properties in pharmacology. Due to the easy handling of synthesis, easily available precursor, and less duration for the reaction, for the synthesis, not many technical skills are needed. All these factors attract chemists to focus more on pyrimidines. Apart from the synthesis of biological applications of pyrimidines, medicinal chemists have gathered to explore more pyrimidine scaffolds due to their interesting medicinal properties and easy targeting of various binding sites. This review delves

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11

West, Thomas P. "Pyrimidine nucleotide synthesis inPseudomonascitronellolis." Canadian Journal of Microbiology 50, no. 6 (2004): 455–59. http://dx.doi.org/10.1139/w04-028.

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Pyrimidine biosynthesis was active in Pseudomonas citronellolis ATCC 13674 and appeared to be regulated by pyrimidines. When wild-type cells were grown on succinate in the presence of uracil, the de novo enzyme activities were depressed while only four enzyme activities were depressed in the glucose-grown cells. On either carbon source, orotic acid-grown cells had diminished aspartate transcarbamoylase, dihydroorotase or OMP decarboxylase activity. Pyrimidine limitation of glucose-grown pyrimidine auxotrophic cells resulted in de novo enzyme activities, except for transcarbamoyolase activity,

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12

Behera, Manoranjan, M. Sambaiah, Poosa Mallesham, et al. "Tandem Schiff-Base Formation/Heterocyclization: An Approach to the Synthesis of Fused Pyrazolo–Pyrimidine/Isoxazolo-Pyrimidine Hybrids." Synlett 30, no. 05 (2019): 586–92. http://dx.doi.org/10.1055/s-0037-1612081.

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A new synthesis of pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines is described. Key steps in the synthesis involve Stille coupling of 4,6-dichloro-2-phenyl-pyrimidine with tributyl(1-ethoxyvinyl)stannane and tandem Schiff-base formation/heterocyclization of 2,6-di-aryl-5-fluoro-4-acetylpyrimidine with hydrazines or hydroxylamine to give pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines, respectively. The position of the fluoro group in the pyrimidine ring is important for the success of heterocylization reaction.

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13

Ogurtsov, Vladimir, and Oleg Rakitin. "4-Chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine." Molbank 2021, no. 3 (2021): M1253. http://dx.doi.org/10.3390/m1253.

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A novel 4-chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine was prepared by a rational and short two-step synthesis from commercially available ethyl 5-amino-1-methyl-1H-pyrazole-4-carboxylate via 6-(chloromethyl)-1-methyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one. The structure of the synthesized compounds was established by elemental analysis, high-resolution mass-spectrometry, 1H, 13C-NMR and IR spectroscopy and mass-spectrometry. 4-Chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine is a convenient intermediate for various disubstituted 1-methyl-1H-pyrazolo[3,4-d]

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14

Abdelhamid, Abdou O., Zeineb H. Ismail, and Anhar Abdel-Aziem. "Reactions with Hydrazonoyl Halides 601: Synthesis of Thieno[2′,3′:4,5] Pyrimidino[1,2-b][1,2,4,5]tetrazines, [1]benzothieno[2′,3′:4,5]pyrimidino [1,2-b][1,2,4,5]tetrazines, Pyrazolo[3′,4′:4,5]pyrimidino[1,2-b] [1,2,4,5]tetrazines and Pyrazolo[3,4-d]pyridazines." Journal of Chemical Research 2007, no. 10 (2007): 609–16. http://dx.doi.org/10.3184/030823407x256118.

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Thieno[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, [1]benzothieno-[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, pyrazolo [3′,4′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, triazolo[4,3- a]pyrimidin-5(1 H)-one, 1-{[2-(1-benzofuran-2-yl)-5-phenyl-4,5-dihydro-1 H-pyrazol-1-yl]-4-substituted-1,3-thiazol-5-yl}-2-phenyldiazene, 3-acyl-4-(1-benzofuran-2-ylcarbonyl) pyrazole and pyrazolo[3,4- d]pyridazine derivatives could be obtained via reactions of hydrazonoyl halides with the appropriate pyrimidine-2-thione, 3-amino-5,6-dimethyl-2-sulfanylthieno[2,3- d]pyrimidin-4(3 H)-one, 5-amino-6-mercapto

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15

Mosaad Sayed Mohamed, Samir Mohamed Awad, Neama Abdallah Abd El-tawab, and Naglaa Mohamed Ahmed. "An overview on synthesis and biological activity of pyrimidines." World Journal of Advanced Research and Reviews 15, no. 1 (2022): 272–96. http://dx.doi.org/10.30574/wjarr.2022.15.1.0689.

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Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 of the six membered ring show wide range of biological activities. Numerous methods for the synthesis of pyrimidine and their diverse reactions offer enormous scope in the field of medicinal chemistry. Pyrimidine possesses wide spectrum of biological activities including antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer, and anti-HIV activity. The present review attempts to give brief information about the synthesis and various biological ac

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16

Murat Saracoglu, Murat Saracoglu, Zulbiye Kokbudak Zulbiye Kokbudak, and M. Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli. "Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives." Journal of the chemical society of pakistan 42, no. 5 (2020): 746. http://dx.doi.org/10.52568/000679.

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Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental

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17

Murat Saracoglu, Murat Saracoglu, Zulbiye Kokbudak Zulbiye Kokbudak, and M. Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli. "Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives." Journal of the chemical society of pakistan 42, no. 5 (2020): 746. http://dx.doi.org/10.52568/000679/jcsp/42.05.2020.

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Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental

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18

Popa, Marcel Mirel, Emilian Georgescu, Mino R. Caira, et al. "Indolizines and pyrrolo[1,2-c]pyrimidines decorated with a pyrimidine and a pyridine unit respectively." Beilstein Journal of Organic Chemistry 11 (June 26, 2015): 1079–88. http://dx.doi.org/10.3762/bjoc.11.121.

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The three possible structural isomers of 4-(pyridyl)pyrimidine were employed for the synthesis of new pyrrolo[1,2-c]pyrimidines and new indolizines, by 1,3-dipolar cycloaddition reaction of their corresponding N-ylides generated in situ from their corresponding cycloimmonium bromides. In the case of 4-(3-pyridyl)pyrimidine and 4-(4-pyridyl)pyrimidine the quaternization reactions occur as expected at the pyridine nitrogen atom leading to pyridinium bromides and consequently to new indolizines via the corresponding pyridinium N-ylides. However, in the case of 4-(2-pyridyl)pyrimidine the steric h

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19

Fawzy, Abdelshafy, M. Barqi Mashael, Ashar Ambreen, Javed Maria, Kanwal Ayesha, and R. Eletmany Mohamed. "Comprehensive Investigation of Pyrimidine Synthesis, Reactions, and Biological Activity." Comprehensive Investigation of Pyrimidine Synthesis, Reactions, and Biological Activity 8, no. 10 (2023): 21. https://doi.org/10.5281/zenodo.10049953.

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Researchers have devoted much attention to the study of the chemistry of pyrimidines due to their broad range of pharmaceutical activities. The important role of pyrimidines in the field of drugs is derived from the fact that they are present in genetic material of cells. In this review, we discuss various synthetic methods for pyrimidine derivatives, as well as their various categories of reactions and biological activities as illustrated by research conducted in recent years.Keywords:- Pyrimidine; Pharmaceutical Activities; Drugs.

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20

Sri Laya A, Govindarao Kamala, Tulasi K, et al. "Current Advances in Synthesis and Therapeutic Applications of Pyrimidine." Journal of Pharma Insights and Research 2, no. 6 (2024): 098–106. https://doi.org/10.69613/v6h5tv11.

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Pyrimidine derivatives are fundamental heterocyclic compounds that serve as essential components of nucleic acids, including uracil, thymine, and cytosine. Modern synthetic approaches for functionalized pyrimidines encompass metal-catalyzed reactions, multicomponent coupling strategies, and green chemistry protocols. The biological significance of pyrimidine scaffolds has led to numerous therapeutic applications across multiple disease states. Pyrimidine-based drugs demonstrate potent antimicrobial effects through antifolate mechanisms, as seen with trimethoprim and pyrimethamine. In antiviral

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21

Chunduru, Jayendra, and Thomas P. West. "Pyrimidine nucleotide synthesis in the emerging pathogen Pseudomonas monteilii." Canadian Journal of Microbiology 64, no. 6 (2018): 432–38. http://dx.doi.org/10.1139/cjm-2018-0015.

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Regulation of pyrimidine biosynthesis by pyrimidines in the emerging, opportunistic human pathogen Pseudomonas monteilii ATCC 700476 was evident. When wild-type cells were grown on succinate in the presence of uracil or orotic acid, the activities of all 5 pyrimidine biosynthetic enzymes were depressed while the activities of 3 of the enzymes decreased in glucose-grown cells supplemented with uracil or orotic acid compared with unsupplemented cells. Pyrimidine limitation of succinate- or glucose-grown pyrimidine auxotrophic cells lacking orotate phosphoribosyltransferase activity resulted in m

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22

Severina, Hanna I., Olga O. Skupa, Natalya I. Voloshchuk, Marharyta M. Suleiman, and Victoriya A. Georgiyants. "Synthesis and anticonvulsant activity of 6-methyl-2-((2-oxo-2-arylethyl)thio)pyrimidin-4(3 H)-one derivatives and products of their cyclization." Pharmacia 66, no. (3) (2019): 141–46. https://doi.org/10.3897/pharmacia.66.e38137.

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The alkylation of 6-methyl-2-thioxo-2,3-dihydro-1H-pyrimidine-4-one phenacyl bromides under different conditions was investigated. It was found that during the reaction in the medium of DMF/K<sub>2</sub>CO<sub>3</sub> a mixture of 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one and 3-hydroxy-3-aryl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-5-one was formed. The holding of the resulting mixture in the concentrated sulphuric acid leads to the formation of cyclization products - derivatives of 3-aryl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one with high yields. Individual S-alkylat

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23

Sarwade, Prakash Pralhad, K. M. Srinandhinidevi, Kiran Dangwal, et al. "Role of Pyrimidine Derivatives in the Treatment of Cancer." Journal for Research in Applied Sciences and Biotechnology 3, no. 5 (2024): 181–93. http://dx.doi.org/10.55544/jrasb.3.5.19.

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The study of the chemistry of pyrimidines is contributing to the expansion of research into the therapeutic applications of these compounds. In the field of medicinal chemistry, the sheer number of pyrimidine synthesis methods and reactions that are available opens up a world of possibilities. These investigations have been inspired by the fact that pyrimidines can be used as building blocks for a wide variety of compounds that have a physiological effect. The pyrimidine ring and its fused derivatives, which include pyrazolo[3,4-d]pyrimidine, pyrido[2,3-d]pyrimidine, quinazoline, and furo[2,3-

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24

Nerkar, A. G., S. A. Ghone, and A. K. Thaker. "In SilicoScreening of the Library of Pyrimidine Derivatives as Thymidylate Synthase Inhibitors for Anticancer Activity." E-Journal of Chemistry 6, no. 3 (2009): 665–72. http://dx.doi.org/10.1155/2009/352717.

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We here report the virtual screening of several series of pyrimidine derivatives forin silicoThymidylate Synthase (TS) inhibition to arrive at possible potential inhibitors of TS with acceptable pharmacokinetic or ADME (Absorption, Distribution, Metabolism and Excretion) properties. Library of the molecules was constructed based upon structural modifications of pyrimidines nucleus. Structural modifications in descending order were performed for the series of pyrimidines,vizfrom pyrimidines with five membered heterocyclic ring to pyrimidines with four membered heterocyclic ring to simple pyrimi

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25

Becker, Sidney, Jonas Feldmann, Stefan Wiedemann, et al. "Unified prebiotically plausible synthesis of pyrimidine and purine RNA ribonucleotides." Science 366, no. 6461 (2019): 76–82. http://dx.doi.org/10.1126/science.aax2747.

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Theories about the origin of life require chemical pathways that allow formation of life’s key building blocks under prebiotically plausible conditions. Complex molecules like RNA must have originated from small molecules whose reactivity was guided by physico-chemical processes. RNA is constructed from purine and pyrimidine nucleosides, both of which are required for accurate information transfer, and thus Darwinian evolution. Separate pathways to purines and pyrimidines have been reported, but their concurrent syntheses remain a challenge. We report the synthesis of the pyrimidine nucleoside

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26

Ahmed Elkanzi, Nadia Ali. "Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review." Oriental Journal Of Chemistry 36, no. 6 (2020): 1001–15. http://dx.doi.org/10.13005/ojc/360602.

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Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and

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27

SABIU RABILU ABDULLAHI, ABUBAKAR MUHD SHAFI’I, SAPNA RAGHAV, and MA’ARUF ABDULMUMIN MUHAMMAD. "Pyrimidine derivatives: Recent discoveries and development towards its medicinal impact." GSC Advanced Research and Reviews 20, no. 1 (2024): 114–28. http://dx.doi.org/10.30574/gscarr.2024.20.1.0248.

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Pyrimidine derivatives' many biological functions and possible therapeutic uses have attracted a lot of research in the field of medicinal chemistry. Recent developments in the synthesis, biological assessment, and therapeutic uses of molecules based on pyrimidines are highlighted in this review. The significance of pyrimidine derivatives in treating a range of ailments, including cancer, infectious diseases, and metabolic disorders, is discussed, along with innovative synthesis approaches and important pharmacological findings. In order to give a thorough picture of the present status of pyri

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SABIU, RABILU ABDULLAHI, MUHD SHAFI'I ABUBAKAR, RAGHAV SAPNA, and ABDULMUMIN MUHAMMAD MA'ARUF. "Pyrimidine derivatives: Recent discoveries and development towards its medicinal impact." GSC Biological and Pharmaceutical Sciences 20, no. 1 (2024): 114–28. https://doi.org/10.5281/zenodo.13640628.

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Pyrimidine derivatives' many biological functions and possible therapeutic uses have attracted a lot of research in the field of medicinal chemistry. Recent developments in the synthesis, biological assessment, and therapeutic uses of molecules based on pyrimidines are highlighted in this review. The significance of pyrimidine derivatives in treating a range of ailments, including cancer, infectious diseases, and metabolic disorders, is discussed, along with innovative synthesis approaches and important pharmacological findings. In order to give a thorough picture of the present status of pyri

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29

Friary, Richard, Andrew T. McPhail, and Vera Seidl. "Novel Syntheses of Tricyclic, N-Aryl, Pyridine- and Pyrazine-Fused Pyrimidones." Collection of Czechoslovak Chemical Communications 58, no. 5 (1993): 1133–50. http://dx.doi.org/10.1135/cccc19931133.

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2-methylthio-2-imidazoline and 2-methylthio-1,4,5,6-tetrahydro-2-pyrimidine amidated 2-chloro-3-pyridine- and 2-chloro-3-pyrazinecarbonyl chlorides. The products reacted with aromatic amines forming a series of tricyclic, linearly fused N-aryl pyrimidones. Included among these pyrimidones were 10-aryl-2,3-dihydroimidazo[1,2-a]pyrido[2,3-d]pyrimidin-5(10H)-ones, 11-aryl-2,3,4,11-tetrahydropyrido-[2,3-d]pyrimido[1,2-a]pyrimidin-6(6H)-ones, 10-aryl-2,3-dihydroimidazo[1,2-a]pyrazino[2,3-d]pyrimidin-5(10H)-ones and 11-aryl-2,3,4,11-tetrahydropyrimido-[1,2-a]pyrazino[2,3-d]pyrimidin-6(6H)-ones. 4,5,

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30

Shevchenko, Nadiya М., Oleksandr O. Severin, Maryna V. Kachaeva, Oleksandr Р. Kozachenko, Yevheniia S. Velihina, and Volodymyr S. Brovarets. "Synthesis of new pyrrolo[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives of piperazin-1-yl-1,3-oxazole-4-carbonitriles, prediction and evaluation of their ADMET properties." Ukrainica Bioorganica Acta 19, no. 2 (2024): 21–32. https://doi.org/10.15407/bioorganica2024.02.021.

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The discovery of nucleoside antibiotics gave impetus to the development of the chemistry of pyrrolo[2,3-d]pyrimidines and thieno[2,3-d]pyrimidines as biologically active compounds. This work describes a universal and efficient approach to the synthesis of new pyrrolo[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives of piperazin-1-yl-1,3-oxazole-4-carbonitriles. Their potential as biologically active compounds is considered and ADMET-score is predicted to assess their further application as pharmaceutical substances

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31

Lee, Su-Jeong, Jun-Gi Ahn, Jihwan Seo, Heun-Jong Ha, and Chang-Woo Cho. "Organocatalytic enantioselective synthesis of acyclic pyrimidine nucleosides by aza-Michael reaction." Organic & Biomolecular Chemistry 16, no. 48 (2018): 9477–86. http://dx.doi.org/10.1039/c8ob02754d.

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32

Pandhurnekar, Chandrashekhar P., Ekta M. Meshram, Himani N. Chopde, and Rameshkumar J. Batra. "Synthesis, Characterization, and Biological Activity of 4-(2-Hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols Derivatives." Organic Chemistry International 2013 (July 1, 2013): 1–10. http://dx.doi.org/10.1155/2013/582079.

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With the aim of synthesizing new heterocyclic compounds and exploring biological potency, new series of chalcones, that is, 3-(2-hydroxy-5-(aryl-diazenyl)phenyl)-1-(aryl)prop-2-en-1-one and their pyrimidine derivatives, that is, 4-(2-hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols were synthesized using different aromatic amines and salicylaldehyde as starting moieties. The structures of newly synthesized compounds were confirmed using different spectroscopic techniques such as IR, 1H-NMR, 13C-NMR, and mass spectral analysis, and elemental analysis. The newly synthesized pyrimidines d

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33

Dawood, Dina H., Eman M. H. Abbas, Thoraya A. Farghaly, Mamdouh M. Ali, and Mohammed F. Ibrahim. "ZnO Nanoparticles Catalyst in the Synthesis of Bioactive Fused Pyrimidines as Anti-breast Cancer Agents Targeting VEGFR-2." Medicinal Chemistry 15, no. 3 (2019): 277–86. http://dx.doi.org/10.2174/1573406414666180912113226.

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Background: Pyrimidines emerged as a remarkable class of heterocyclic compounds that have reinforced the pharmaceutical chemistry with various bioactive antitumor agents. Moreover, pyrimidine scaffold displayed VEGFR-2 inhibitory activity. Also, nano-sized catalysts are used in organic reactions in order to speed up the catalytic process. Objective: We were interested herein to synthesize a new series of fused pyrimidines using ZnO(NPs) to investigate their antitumor efficiency against breast MCF7 cancer and their VEGFR- 2 inhibition properties. Method: A simple and efficient method for the sy

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Edrees, Mastoura M. "Synthesis of 4-hydrazinopyrazolo[3,4-d]pyrimidines and their Reactions with Carbonyl Compounds." Journal of Chemical Research 37, no. 1 (2013): 6–10. http://dx.doi.org/10.3184/174751912x13543818811749.

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Synthesis of a new 4-hydrazinopyrazolo[3,4- d]pyrimidine was achieved via heating (4,6-dithioxo-1 H-pyrazolo[3,4- d] pyrimidin-3-yl)acetonitrile with hydrazine hydrate. Reactions of the latter product with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues afforded the corresponding hydrazone and pyrazole derivatives, respectively. Similarly, condensation of 2-[6-(benzylsulfanyl)-4-hydrazino-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues gave the respective hydrazone and pyrazolone derivatives. Alkylation

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35

Dabaeva, V. V., M. R. Baghdasaryan, I. M. Barkhudaryants, E. G. Paronikyan, and Sh Sh Dashyan. "Synthesis of new fused 3(4)-substituted 11-furylthieno[3,2-<i>d</i>]pyrimidine derivatives." Журнал общей химии 93, no. 9 (2023): 1351–57. http://dx.doi.org/10.31857/s0044460x23090056.

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A method was developed for the synthesis of new fused 3-alkyl-substituted derivatives of thieno[3,2- d ]pyrimidin-4(3 H )-ones based on 11-(2-furyl)-8,8-dimethyl-7,10-dihydro-8 H -pyrano[3′′,4′′:5′,6′]pyrido[3′,2′:4,5]-thieno[3,2- d ]pyrimidin-4(3 H )-one via nucleophilic substitution in the pyrimidine ring. A series of fused 4-amino-substituted 11-furylthieno[3,2- d ]pyrimidine derivatives was also synthesized from the corresponding 4-chloro derivative.

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36

Kumar, Sanjiv, Aakash Deep, and Balasubramanian Narasimhan. "A Review on Synthesis, Anticancer and Antiviral Potentials of Pyrimidine Derivatives." Current Bioactive Compounds 15, no. 3 (2019): 289–303. http://dx.doi.org/10.2174/1573407214666180124160405.

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Background: Pyrimidine is the six membered heterocyclic aromatic compound similar to benzene and pyridine containing two nitrogen atoms at 1st and 3rd positions. Pyrimidine is present throughout nature in various forms and is the building blocks of numerous natural compounds from antibiotics to vitamins and liposacharides. The most commonly recognized pyrimidines are the bases of RNA and DNA, the most abundant being cytosine, thymine or uracil. Results: Pyrimidine is a core structure in a wide variety of compounds that exhibits significant biological activity and also plays an important role i

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37

Hussein, Khlood Abdulla Ahmed, and Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine." University of Aden Journal of Natural and Applied Sciences 25, no. 2 (2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted

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38

Hussein, Khlood Abdulla Ahmed, and Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine." University of Aden Journal of Natural and Applied Sciences 25, no. 2 (2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted

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39

Povidaichyk, M., О. Onysko, and M. Onysko. "SYNTHESIS OF TERMINAL 2-ALKENYL(ALKYNYL)THIO-5-CYANO-6-(p-DIMETHYLAMINOPHENYL)PYRIMIDIN-4-ONES." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 48, no. 2 (2023): 79–83. http://dx.doi.org/10.24144/2414-0260.2022.2.79-83.

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Functionalized pyrimidines possess a wide spectrum of biological activity. In particular, they have antitumor, antiviral, and anticonvulsant activities, exhibit anti-inflammatory and analgesic effects, and they are inhibitors of aldose reductase, SecA ATPase, azide, and plant growth. The search for methods of synthesis of new functionalized and condensed pyrimidine derivatives is an urgent problem. Alkenyl-functionalized mono- and polycyclic pyrimidines are promise substrates for studying the regioselectivity of electroph ilic heterocyclization reactions under the influence of halogen-co

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40

Mamaghani, Manouchehr. "Ultrasound-promoted synthesis of novel dihydropyrido[2,3-d:5,6- d`]dipyrimidine derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 11, no. 5 (2015): 3567–75. http://dx.doi.org/10.24297/jac.v11i5.4475.

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An efficient synthesis of dihydropyrido[2,3-d:5,6-d`]pyrimidine derivatives was developed via one-pot three-component reaction of 6-amino-2-(alkylthio)-pyrimidine-4(3H)one and aryl aldehydes in the mixed solvent of glacial acetic acid and DMF (1:1, v:v) under ultrasonic irradiation. In this protocol novel fused dihydropyrido[2,3-d]pyrimidines were synthesized in high yields (80-97%) and lower reaction times (5-25 min).

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41

Amatur, Roquia, and tam Tilak. "Design and Synthesis of Novel Chromeno Pyrimidine analogs of potential Antimicrobial properties." International Journal of Applied Sciences and Management 1, no. 2 (2016): 105–16. https://doi.org/10.5281/zenodo.5172238.

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The aim of the study is to design and synthesize the new bioactive heterocyclic compounds. Pyrimidine is an important class of heterocyclic compound that are known to possess important pharmacological and antimicrobial properties. 2H-chromenes are also known to possess antimicrobial properties. Chromeno pyrimidines are compounds having both pyrimidines and 2H-chromenes in their structures. Hence, the synthesis of novel chromeno pyrimidine containing chloro, fluoro, trifluoromethyl groups have been carried out by multi-step organic synthesis, in order to study their interesting antimicrobial pr

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42

Latif, Muhammad, Byung Jin Byun, and Kwangho Lee. "Synthesis of 4‐(3,4‐dicarboxamido‐1H‐pyrrole)pyrimidines as Anaplastic Lymphoma Kinase Inhibitors." Bulletin of the Korean Chemical Society 36, no. 2 (2015): 520–25. http://dx.doi.org/10.1002/bkcs.10097.

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To explore non‐aniline aromatic substitution on the pyrimidine C4 position, novel 4‐(N,N′‐di‐n‐propyl‐3,4‐dicarboxamido‐1H‐pyrrole)pyrimidines are designed and synthesized as anaplastic lymphoma kinase inhibitors for non‐small cell lung cancer treatment. To overcome the unexpected cleavage between the C‐N linkage of pyrrole nitrogen and C4‐pyrimidine during hydrolysis and inaccessibility of the desired diamide formation through coupling agent‐mediated conditions, the 4‐(N,N′‐di‐n‐propyl‐3,4‐dicarboxamido‐1H‐pyrrole)pyrimidine was assembled through direct nucleophilic substitution under microwa

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Mohamed, Mosaad, Ramdan El-Domany, and Rania Abd El-Hameed. "Synthesis of certain pyrrole derivatives as antimicro-bial agents." Acta Pharmaceutica 59, no. 2 (2009): 145–58. http://dx.doi.org/10.2478/v10007-009-0016-9.

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Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds

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44

Mamaghani, M., K. Tabatabaeian, R. Araghi, A. Fallah, and R. Hossein Nia. "An Efficient, Clean, and Catalyst-Free Synthesis of Fused Pyrimidines Using Sonochemistry." Organic Chemistry International 2014 (November 16, 2014): 1–9. http://dx.doi.org/10.1155/2014/406869.

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In this report, synthesis of indenopyrido[2,3-d]pyrimidine and pyrimido[4,5-b]quinoline derivatives was investigated via one-pot three-component reaction between 6-amino-2-(alkylthio)-pyrimidin-4(3H)one, 1,3-indanedione, or 1,3-cyclohexadione and arylaldehyde under ultrasonic irradiation in ethylene glycol as solvent at 65°C. In these reactions fused pyrimidine derivatives were synthesized with high to excellent yields (82–97%) and short reaction times (10–33 min).

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45

Tank, Manishkumar Jinabhai, Navinkumar A. Kucha, Chirag G. Naik, Tina R. Barot, and G. M. Malik. "Adamantane-pyrido[2,3-d]pyrimidine Derivatives; Synthesis, Characterization and Investigation of Antimicrobial Study." Oriental Journal Of Chemistry 39, no. 2 (2023): 393–402. http://dx.doi.org/10.13005/ojc/390219.

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Target molecules based on Adamantane-pyrido[2,3-d]pyrimidine derivatives were prepared. Adamantane-pyrido[2,3-d]pyrimidine series using N-(hydroxyadamantan-1-yl)-5-(2,4-substitutedphenyl)-2-Methyl-4-Oxo-7-(2-oxo-2H-Chromen-3-yl)pyrido[2,3-d]Pyrimidine-3(4H)carboxamide (6a-j) was synthesized by reaction between 3-(2-chloroacetyl)-5-(2,4-substitutedphenyl)-2-Methyl-7-(2-Oxo-2H-Chromen-3-yl) pyrido[2,3-d]pyrimidin-4(3H)-one (5a-j) and 3-aminoadamantan-1-ol. These derivatives of Adamantane-pyrido[2,3-d]Pyrimidine were investigated in vitro for their biological characteristics against the strains w

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46

Journal, Baghdad Science. "Synthesis of Some Heterocyclic Compounds derived from 2-mercapto pyrimidine." Baghdad Science Journal 7, no. 2 (2010): 1014–22. http://dx.doi.org/10.21123/bsj.7.2.1014-1022.

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In this work 2-hydrazino pyrimidine (1) was prepared from 2-mercapto pyrimidine with hydrazine hydrate. Treatment of (1) with active methylene compounds gave 2-(3,5-dimethyl -1 H – Pyrazole-1-yl) pyrimidine , whereas the reaction of (1) with carboxylic anhydride namely maleic anhydride or 1,2,3,6-tetra hydro phthalic anhydride yielded 1-Pyrimidine-2-yl-1,2-dihydro pyridazine-3,6-dione (3) and 2 – Pyrimidin -2-yl -2,3,4 a ,5,8 a – hexahydro phthalazine 1,4 – dione (4) . Reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-Phenyl-1,3-thiazolidine-2,4-dione-2( pyrimidine

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47

Askar, Firyal w., Huda A. Hassan, and Nahida A. Jinzeel. "Synthesis of Some Heterocyclic Compounds derived from 2-mercapto pyrimidine." Baghdad Science Journal 7, no. 2 (2010): 1014–22. http://dx.doi.org/10.21123/bsj.2010.7.2.1014-1022.

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In this work 2-hydrazino pyrimidine (1) was prepared from 2-mercapto pyrimidine with hydrazine hydrate. Treatment of (1) with active methylene compounds gave 2-(3,5-dimethyl -1 H – Pyrazole-1-yl) pyrimidine , whereas the reaction of (1) with carboxylic anhydride namely maleic anhydride or 1,2,3,6-tetra hydro phthalic anhydride yielded 1-Pyrimidine-2-yl-1,2-dihydro pyridazine-3,6-dione (3) and 2 – Pyrimidin -2-yl -2,3,4 a ,5,8 a – hexahydro phthalazine 1,4 – dione (4) . Reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-Phenyl-1,3-thiazolidine-2,4-dione-2( pyrimidine

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48

Geies, Ahmed A. "Bromonitriles in Heterocyclic Synthesis. Synthesis and Reactions of Thiazolo[3,2-a]pyrimidines (III)." Collection of Czechoslovak Chemical Communications 57, no. 7 (1992): 1565–69. http://dx.doi.org/10.1135/cccc19921565.

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As a continuation of our previous work about the synthesis and properties of thiazolopyrimidines, which are expected to be of biological and medicinal importance, the present work is aimed to synthesize new polyfunctional substituted thiazolo[3,2-a]pyrimidines. Pyrimidine derivatives I were reacted with bromomalononitrile or ethyl bromocyanoacetate at room temperature in ethanol in presence of potassium hydroxide as a basic catalyst followed by refluxing the reaction mixture to give thiazolo[3,2-a]pyrimidines IIa-IId.

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49

Velihina, Y. S., S. G. Pilyo, I. V. Ivanova, and V. S. Brovarets. "Synthesis of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives and study of their vasodilator activity." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 2 (May 2023): 51–60. http://dx.doi.org/10.32434/0321-4095-2023-147-2-51-60.

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A number of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives were synthesized and characterized. Pyrazolo[1,5-a][1,3,5]triazines with various substituents in the fourth position and a dichloromethyl group in the second position were obtained by the heterocyclization reaction of available N-(2,2-dichloro-1-cyanoethenyl)carboxamides and 5-aminopyrazoles. Oxazolo[4,5-d]pyrimidines were obtained by treating 2-phenyl-4-dichloromethylene-1,3-oxazol-5(4H)-one with the corresponding arylamidine hydrochloride in the presence of triethylamine. The resulting 4,5-dihydro-1H-imidazol

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50

Huppatz, JL. "Systemic Fungicides. The Synthesis of Pyrazolo[1,5-a]pyrimidine Analogues of Carboxin." Australian Journal of Chemistry 38, no. 1 (1985): 221. http://dx.doi.org/10.1071/ch9850221.

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The synthesis of a series of pyrazolo [1,5-a] pyrimidine derivatives, structural analogues of the systemic fungicide carboxin, is described. A common intermediate incorporating structural features desirable for fungicidal activity, N-phenyl-3(5)-amino-5(3)-methylpyrazole-4- carboxamide (6), was used to prepare pyrazolo [1,5-a] pyrimidines variously substituted in positions 5 and 7 of the ring system. Bromination of N-phenyl-2-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide (8) occurred preferentially in the phenyl ring and the 6-bromo derivative was prepared by bromination of the corresponding 3

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