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Journal articles on the topic 'Pyrimidmes'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

KRISHNA, C. JOSHI, N. PATHAK VIJAI, and GUPTA RAGINI. "Reactions of 2-(FIuoroaryl)-lH-indole-3- carboxaldehydes with Barbituric and Thiobarbituric Acids." Journal of Indian Chemical Society Vol. 67, May 1990 (1990): 434–35. https://doi.org/10.5281/zenodo.6280122.

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Department of Chemistry, University of Rajasthan, Jaipur-302 004 Manuscript received 5 September 1988, revised 28 December 1989, accepted 1 January 1990 Reactions of 2-(Fluoroaryl)-lH-indole-3- carboxaldehydes with Barbituric and Thiobarbituric Acids     

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2

García-García, Ángela, Jesus Vicente de Julián-Ortiz, Jorge Gálvez, et al. "Similarity-Based Virtual Screening to Find Antituberculosis Agents Based on Novel Scaffolds: Design, Syntheses and Pharmacological Assays." International Journal of Molecular Sciences 23, no. 23 (2022): 15057. http://dx.doi.org/10.3390/ijms232315057.

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A method to identify molecular scaffolds potentially active against the Mycobacterium tuberculosis complex (MTBC) is developed. A set of structurally heterogeneous agents against MTBC was used to obtain a mathematical model based on topological descriptors. This model was statistically validated through a Leave-n-Out test. It successfully discriminated between active or inactive compounds over 86% in database sets. It was also useful to select new potential antituberculosis compounds in external databases. The selection of new substituted pyrimidines, pyrimidones and triazolo[1,5-a]pyrimidines

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3

Al-Azmi, Amal. "Novel 6-substituted Pyrimidines and Pyrimido[5,4-d]pyrimidines from (2-acetamido-1,2-dicyanovinyl)Ammonium Chloride." Journal of Chemical Research 2005, no. 8 (2005): 530–34. http://dx.doi.org/10.3184/030823405774663200.

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The reaction of triethyl orthoformate with 5-amino-6-ethoxy-2-methyl-4-pyrimidinecarbonitrile (5), available from DAMN via the ammonium salt 4, afforded iminoformate 6. The latter cyclised with aqueous ammonia or equimolar amounts of aryl/benzyl amines to give the corresponding pyrimido[5,4-d]pyrimidines 8, 9a–c. Reaction with excess of aqueous ethylamine, methylamine or benzylamine caused cyclisation with substitution of an ethoxy group to give 9d–f. Hydrolysis of compounds 8, 9a–b under acidic conditions gave the corresponding pyrimido[5,4-d]pyrimidones 10, 11a–b. Heating 4 to reflux in THF

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4

Uryadova, Anastasia, Elena Makarova, and Sergey Filimonov. "Diastereoselective synthesis of chromeno[4,3-d]pyrimidines." From Chemistry Towards Technology Step-By-Step 4, no. 2 (2023): 66–71. http://dx.doi.org/10.52957/2782-1900-2024-4-2-66-71.

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The paper investigates the diastereoselective synthesis of chromeno[4,3-d]pyrimidines by isolation and cyclization of diastereomerically pure dihydropyrimidine addition intermediates to resorcinol. The authors discovered the reversibility of the addition reaction to be an important factor that could neutralize the dominant formation of one of the intermediate diastereomers.

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5

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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6

Chebanov, Valentin A., Vyacheslav E. Saraev, Ekaterina A. Gura, Sergey M. Desenko та Vladimir I. Musatov. "Some Aspects of Reaction of 6-Aminouracil and 6-Amino-2-Thiouracil with α,β-Unsaturated Ketones". Collection of Czechoslovak Chemical Communications 70, № 3 (2005): 350–60. http://dx.doi.org/10.1135/cccc20050350.

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A number of 5,7-diaryl-5,8-dihydropyrido[2,3-d]pyrimidines and 5,7-diarylpyrido[2,3-d]- pyrimidines were obtained by the reaction of 6-aminouracil derivatives with α,β-unsaturated ketones. Basic catalysts decrease yields of the dihydro derivatives whereas acids increase it. In the reactions of ketones containing the dimethylamino group, elimination of the aryl substituent from position 5 of the pyridopyrimidine system was observed. Some aspects of oxidation of 5,8-dihydropyrido[2,3-d]pyrimidines and synthesis of pyrido[2,3-d]pyrimidines were also investigated.

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7

Agarkov, A. S., A. K. Shiryaev, S. E. Solovieva, and I. S. Antipin. "Synthesis, chemocal properties and application of 2-substituted derivatives of thiazolo[3,2-<i>a</i>]pyrimidine." Журнал органической химии 59, no. 3 (2023): 285–315. http://dx.doi.org/10.31857/s0514749223030011.

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The review describes in detail the methods of obtaining thiazolo[3,2- a ]pyrimidines, synthesis and chemical properties of 2-substituted derivatives of thiazolo[3,2- a ]pyrimidines, analysis of crystal structures of 2-arylmethylidene derivatives of thiazolo[3,2- a ]pyrimidines and demonstrates their high antitumor, antibacterial and anti-inflammatory activity.

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8

Campos, Joana F., Thierry Besson, and Sabine Berteina-Raboin. "Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives." Pharmaceuticals 15, no. 3 (2022): 352. http://dx.doi.org/10.3390/ph15030352.

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The objective of this review is to list the structures composed of a pyridopyrimidine moiety which have shown a therapeutic interest or have already been approved for use as therapeutics. We consider all the synthetic protocols to prepare these pyridopyrimidine derivatives. The review is organized into four sections, successively pyrido[2,3-d]pyrimidines, pyrido[3,4-d]pyrimidines, pyrido[4,3-d]pyrimidines and pyrido[3,2-d]pyrimidines. For each compound we present the biological activity and the synthetic route reported. To produce this manuscript, the bibliographic research was done using Reax

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9

Ofitserova, Ekaterina S., Lilia N. Alekseeva, Artem A. Shklyarenko, and Igor P. Yakovlev. "Biological activity of new 6-[(1-naphthylmethyl)thio)]-4-chloropyrazolo[3,4-d]pyrimidines." Aspirantskiy Vestnik Povolzhiya 20, no. 1-2 (2020): 146–51. http://dx.doi.org/10.17816/2072-2354.2020.20.1.146-151.

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Topicality. This article presents the results of the study of the biological activity of newly synthesized 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines. The acute toxicity of 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines was determined experimentally on non-linear white male mice with a total weight of 1620 g. A generation model was used to experimentally evaluate the analgesic activity acetic writhing in male mice. It was experimentally confirmed that the new synthesized 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines were non-toxic and had prono

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10

Liu, Xianxian, and Rebecca E. Parales. "Chemotaxis of Escherichia coli to Pyrimidines: a New Role for the Signal Transducer Tap." Journal of Bacteriology 190, no. 3 (2007): 972–79. http://dx.doi.org/10.1128/jb.01590-07.

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ABSTRACT Escherichia coli exhibits chemotactic responses to sugars, amino acids, and dipeptides, and the responses are mediated by methyl-accepting chemotaxis proteins (MCPs). Using capillary assays, we demonstrated that Escherichia coli RP437 is attracted to the pyrimidines thymine and uracil and the response was constitutively expressed under all tested growth conditions. All MCP mutants lacking the MCP Tap protein showed no response to pyrimidines, suggesting that Tap, which is known to mediate dipeptide chemotaxis, is required for pyrimidine chemotaxis. In order to confirm the role of Tap

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11

B., SRINIVAS, and SRINIVASULU K. "Separation of some Purines and Pyrimidines by Thin Layer Chromatography using Heulandite as an Adsorbent." Journal of Indian Chemical Society Vol. 71, Nov 1994 (1994): 711–12. https://doi.org/10.5281/zenodo.5897777.

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School of Studies in Chemistry, Vikram University, Ujjain-456 010 <em>Manuscript received 15 March 1993, revised 16 July 1993, accepted 30 July 1993</em> Separation of some Purines and Pyrimidines by Thin Layer Chromatography using Heulandite as an Adsorbent.

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12

Al-Zaydi, Khadijah Mohamed, Mariam Abd Alha Al-Shiekh, and Ebtisam Abdel-Aziz Hafez. "Enaminonitriles in Heterocyclic Synthesis: New Routes for the Synthesis of Some Novel Azolo[1,5-a]pyrimidine, Pyrimido[1,2-a]benzimidazole, Pyrido[1,2-a]benimdazole, Pyrazolo[3,4-b]pyridine, Pyrazole and Pyrimidine Derivatives." Journal of Chemical Research 2000, no. 1 (2000): 13–15. http://dx.doi.org/10.3184/030823400103165716.

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13

Monier, M., Doaa Abdel-Latif, Ahmed El-Mekabaty, and Khaled M. Elattar. "Bicyclic 6 + 6 systems: the chemistry of pyrimido[4,5-d]pyrimidines and pyrimido[5,4-d]pyrimidines." RSC Advances 9, no. 53 (2019): 30835–67. http://dx.doi.org/10.1039/c9ra05687d.

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The present investigation provides an overview of the chemistry of pyrimido[4,5-d]pyrimidines and pyrimido[5,4-d]pyrimidines. The synthetic methods, reactivities, and biological applications are described.

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14

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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15

Goswami, Shyamaprosad, Subrata Jana, Swapan Dey, and Avijit Kumar Adak. "Microwave-Expedited One-Pot, Two-Component, Solvent-Free Synthesis of Functionalized Pyrimidines." Australian Journal of Chemistry 60, no. 2 (2007): 120. http://dx.doi.org/10.1071/ch06388.

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The synthesis of a series of diversely substituted pyrimidines under solvent-free conditions in good yields is described. Under microwave irradiation, a variety of nucleophilic substrates containing the N–C–N unit with β-dicarbonyl compounds, ethyl cyanoacetate, malononitrile, and chalcones was cyclized to give pyrimidines. A combinatorial type approach for a one-step synthesis has been developed where a ring-closing condensation is followed by spontaneous aromatization to afford 28 functionalized and aryl/alkyl substituted pyrimidines.

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16

Gorja, Dhilli Rao, K. Shiva Kumar, K. Mukkanti, and Manojit Pal. "C–C (alkynylation) vs C–O (ether) bond formation under Pd/C–Cu catalysis: synthesis and pharmacological evaluation of 4-alkynylthieno[2,3-d]pyrimidines." Beilstein Journal of Organic Chemistry 7 (March 21, 2011): 338–45. http://dx.doi.org/10.3762/bjoc.7.44.

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The Pd/C–CuI–PPh3 catalytic system facilitated C–C bond formation between 4-chlorothieno[2,3-d]pyrimidines and terminal alkynes in methanol with high selectivity without generating any significant side products arising from C–O bond formation between the chloro compounds and methanol. A variety of novel 4-alkynylthieno[2,3- d]pyrimidines were prepared via alkynylation of 4-chlorothieno[2,3-d]pyrimidines in good to excellent yields. Some of the compounds synthesized were tested for cytotoxic activity in vitro.

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17

Elnagdi, Mohamed Hilmy, Nadia Hassen Taha, Fatma Abdel Maksoud Abd El All, Ramadan Maawad Abdel-Motaleb, and Fivian Farouk Mahmoud. "Studies on condensed pyrazoles: Synthesis of new methyl and amino pyrazolo[1,5-a]pyrimidines and of pyrazolo[5,1-c][1,2,4]triazines." Collection of Czechoslovak Chemical Communications 54, no. 4 (1989): 1082–91. http://dx.doi.org/10.1135/cccc19891082.

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A variety of 3-arylazo 5-amino and 7-aminopyrazolo[1,5-a]pyrimidines were obtained via reacting Ia-Id with cinnamonitriles. The structure of products was confirmed via 1H NMR. Both 5-amino- and 7-amino-3-arylazo pyrazolo[1,5-a]pyrimidines reacted, with protons in acetic acid-sulphuric acid mixture to yield the corresponding 3-unsubstituted acetylaminopyrazolo[1,5-a]pyrimidines. Diazotized Ia and Ib coupled with a variety of active methylene reagents to yield pyrazolo[5,1-c][1,2,4]triazines.

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18

Abhishek, S. Saxena, Goel Atul, and Ji Ram Vishnu. "A convenient and expwitious synthesis of annulated N, S-heterocycles." Journal of Indian Chemical Society Vol. 80, Apr 2003 (2003): 311–18. https://doi.org/10.5281/zenodo.5839578.

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Medicinal Chemistry Division, Central Drug Research ln$titute, Lucknow-226 001, India E-mail : vjiram@yahoo.com_ Fax: 91-522-223405 <em>Manuscript received 19 September 2002</em> A convenient synthesis of titiett[2,3-<em>b</em>]pyridines (3), thieno[3,2-<em>c</em>]pxridines (4), pyrazolo[3,4-<em>b</em>]ipyridines (6), thieno[2,3- <em>d</em>]pyrimidines (9), pyridoll,2-althienol2,3-dlpyrimidines (11), pyrido[1,2-<em>a</em>]pyrimido141,51 : 4,5[thien:o[2,3-<em>d</em>]pyrimidines (12), pyrido[1,2-<em>a</em>]pyrimido[4,5-<em>d</em>]pyiimidines (13) and pyrazolor[3,4-<em>d</em>]pyrimido[1,2-a]pyrim

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19

Jamasbi, N., M. Irankhah-Khanghah, F. Shirini, H. Tajik, and M. S. N. Langarudi. "DABCO-based ionic liquids: introduction of two metal-free catalysts for one-pot synthesis of 1,2,4-triazolo[4,3-a]pyrimidines and pyrido[2,3-d]pyrimidines." New Journal of Chemistry 42, no. 11 (2018): 9016–27. http://dx.doi.org/10.1039/c8nj01455h.

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In this study, structurally functionalized 1,2,4-triazolo[4,3-a]pyrimidines and pyrido[2,3-d]pyrimidines were synthesized by two non-metal DABCO-based ionic liquids which were compared in catalytic activity in both reactions.

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20

Jismy, Badr, Mohamed Akssira, Damijan Knez, Gérald Guillaumet, Stanislav Gobec, and Mohamed Abarbri. "Efficient synthesis and preliminary biological evaluations of trifluoromethylated imidazo[1,2-a]pyrimidines and benzimidazo[1,2-a]pyrimidines." New Journal of Chemistry 43, no. 25 (2019): 9961–68. http://dx.doi.org/10.1039/c9nj01982k.

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Fluoromethylated imidazo[1,2-a]pyrimidines and benzimidazo[1,2-a]pyrimidines were synthesized through Michael addition/intramolecular cyclization reaction by condensation of 2-amino imidazole derivatives with ethyl 4,4,4-trifluorobut-2-ynate and using C–O bond activation.

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21

Ofitserova, E. S., L. N. Alekseeva, A. A. Shklyarenko, and I. P. Yakovlev. "Biological Activity of New 1-Benzoyl-Subctituted 6-(Methylthio)-4-Chloro-1h-Pyrazolo[3,4-D]Pyrimidines." Medicina 8, no. 3 (2020): 76–84. http://dx.doi.org/10.29234/2308-9113-2020-8-3-76-84.

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The article presents results of the study of the biological activity of newly synthesized 1-benzoyl-substituted-6- (methylthio) -4-chloro-1H-pyrazolo [3,4-d] pyrimidines. The acute toxicity of 2-aryl-6- (methylthio) -4-chloro-2H-pyrazolo [3,4-d] pyrimidines was determined experimentally on non-linear white male mice with a total weight of 16-20 g. A generation model was used to experimentally evaluate the analgesic activity acetic "writhing" in mice. It was experimentally confirmed that the synthesized new 2-aryl-6- (methylthio) -4-chloro-2H-pyrazolo [3,4-d] pyrimidines are non-toxic and have

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22

Greco, Chiara, Rosa Catania, Dario Leonardo Balacco, et al. "Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors." Molecules 25, no. 22 (2020): 5354. http://dx.doi.org/10.3390/molecules25225354.

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Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. Here, we explored the activity of a library of in-house pyrazolo[3,4-d]pyrimidines, targeting human protein kinases, against Staphylococcus aureus and Escherichia coli and their interaction with ampicillin and kanamycin, representing important classes of clinically used antibiotics. Our results repre

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23

Szennyes, Eszter, Gyöngyi Gyémánt, László Somsák та Éva Bokor. "Synthesis of New Series of 2-C-(β-D-glucopyranosyl)-Pyrimidines and Their Evaluation as Inhibitors of Some Glycoenzymes". Molecules 25, № 3 (2020): 701. http://dx.doi.org/10.3390/molecules25030701.

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Despite the substantial interest in C-glycosyl heterocycles as mimetics of biologically active native glycans, the appearance of C-glycopyranosyl derivatives of six-membered heterocycles, both in synthetic and biological contexts, is rather scarce. As part of our ongoing research program aimed at preparing hitherto barely known 2-C-glycopyranosyl pyrimidines, the goal of the present study was to synthesize new 5-mono- and multiply substituted derivatives of this compound class. Thus, 2-C-(β-D-glucopyranosyl)-5,6-disubstituted-pyrimidin-4(3H)-ones and 4-amino-2-C-(β-D-glucopyranosyl)-5,6-disubs

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24

Naglah, Ahmed M., Ahmed A. Askar, Ashraf S. Hassan, Tamer K. Khatab, Mohamed A. Al-Omar, and Mashooq A. Bhat. "Biological Evaluation and Molecular Docking with In Silico Physicochemical, Pharmacokinetic and Toxicity Prediction of Pyrazolo[1,5-a]pyrimidines." Molecules 25, no. 6 (2020): 1431. http://dx.doi.org/10.3390/molecules25061431.

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Pyrazolo[1,5-a]pyrimidines 5a–c, 9a–c and 13a–i were synthesized for evaluation of their in vitro antimicrobial properties against some microorganisms and their immunomodulatory activity. The biological activities of pyrazolo[1,5-a]pyrimidines showed that the pyrazolo[1,5-a]pyrimidines (5c, 9a, 9c, 13a, 13c, 13d, 13e and 13h) displayed promising antimicrobial and immunomodulatory activities. Studying the in silico predicted physicochemical, pharmacokinetic, ADMET and drug-likeness properties for the pyrazolo[1,5-a]pyrimidines 5a–c, 9a–c and 13a–i confirmed that most of the compounds (i) were w

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Vaghasia, S. J., and V. H. Shah. "Microwave assisted synthesis and antimicrobial activity of some novel pyrimidine derivatives." Journal of the Serbian Chemical Society 72, no. 2 (2007): 109–17. http://dx.doi.org/10.2298/jsc0702109v.

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The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidi

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Wang, Y. C., V. M. Maher, D. L. Mitchell, and J. J. McCormick. "Evidence from mutation spectra that the UV hypermutability of xeroderma pigmentosum variant cells reflects abnormal, error-prone replication on a template containing photoproducts." Molecular and Cellular Biology 13, no. 7 (1993): 4276–83. http://dx.doi.org/10.1128/mcb.13.7.4276-4283.1993.

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Xeroderma pigmentosum (XP) variant patients are genetically predisposed to sunlight-induced skin cancer. Fibroblasts derived from these patients are extremely sensitive to the mutagenic effect of UV radiation and are abnormally slow in replicating DNA containing UV-induced photoproducts. However, unlike cells from the majority of XP patients, XP variant cells have a normal or nearly normal rate of nucleotide excision repair of such damage. To determine whether their UV hypermutability reflected a slower rate of excision of photoproducts specifically during early S phase when the target gene fo

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Wang, Y. C., V. M. Maher, D. L. Mitchell, and J. J. McCormick. "Evidence from mutation spectra that the UV hypermutability of xeroderma pigmentosum variant cells reflects abnormal, error-prone replication on a template containing photoproducts." Molecular and Cellular Biology 13, no. 7 (1993): 4276–83. http://dx.doi.org/10.1128/mcb.13.7.4276.

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Xeroderma pigmentosum (XP) variant patients are genetically predisposed to sunlight-induced skin cancer. Fibroblasts derived from these patients are extremely sensitive to the mutagenic effect of UV radiation and are abnormally slow in replicating DNA containing UV-induced photoproducts. However, unlike cells from the majority of XP patients, XP variant cells have a normal or nearly normal rate of nucleotide excision repair of such damage. To determine whether their UV hypermutability reflected a slower rate of excision of photoproducts specifically during early S phase when the target gene fo

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Lagardère, Prisca, Cyril Fersing, Nicolas Masurier, and Vincent Lisowski. "Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents." Pharmaceuticals 15, no. 1 (2021): 35. http://dx.doi.org/10.3390/ph15010035.

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Thienopyrimidines are widely represented in the literature, mainly due to their structural relationship with purine base such as adenine and guanine. This current review presents three isomers—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—and their anti-infective properties. Broad-spectrum thienopyrimidines with biological properties such as antibacterial, antifungal, antiparasitic and antiviral inspired us to analyze and compile their structure–activity relationship (SAR) and classify their synthetic pathways. This review explains the main access route to syn

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29

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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30

Sahu, Umakant, Elodie Villa, Colleen R. Reczek, et al. "Pyrimidines maintain mitochondrial pyruvate oxidation to support de novo lipogenesis." Science 383, no. 6690 (2024): 1484–92. http://dx.doi.org/10.1126/science.adh2771.

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Cellular purines, particularly adenosine 5′-triphosphate (ATP), fuel many metabolic reactions, but less is known about the direct effects of pyrimidines on cellular metabolism. We found that pyrimidines, but not purines, maintain pyruvate oxidation and the tricarboxylic citric acid (TCA) cycle by regulating pyruvate dehydrogenase (PDH) activity. PDH activity requires sufficient substrates and cofactors, including thiamine pyrophosphate (TPP). Depletion of cellular pyrimidines decreased TPP synthesis, a reaction carried out by TPP kinase 1 (TPK1), which reportedly uses ATP to phosphorylate thia

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Al-Azmi, Amal. "Pyrazolo[1,5-a]pyrimidines: A Close Look into their Synthesis and Applications." Current Organic Chemistry 23, no. 6 (2019): 721–43. http://dx.doi.org/10.2174/1385272823666190410145238.

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Pyrazolo[1,5-a]pyrimidines are fused N-heterocyclic systems of a pyrazole. They are considered as a key structural motif in many vital applications, such as medicinal, pharmaceuticals, pesticides, dyes and pigments. Their synthetic routes have escalated dramatically in the last decades. The current review is a recent synthetic survey of pyrazolo[ 1,5-a]pyrimidines and their applications until recently.

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32

Hocková, Dana, Milena Masojídková, and Antonín Holý. "Sonogashira Cross-Coupling in the Synthesis of Acyclic Nucleoside Phosphonates: Preparation of 6-[(Phosphonomethoxy)alkynyl]- and 6-[(Phosphonomethoxy)alkyl]pyrimidines." Collection of Czechoslovak Chemical Communications 70, no. 2 (2005): 247–58. http://dx.doi.org/10.1135/cccc20050247.

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Several 6-[(phosphonomethoxy)alkyl]pyrimidines and 6-[(phosphonomethoxy)alkynyl]pyrimidines were prepared as saturated and unsaturated carba-analogues of antivirally active 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidine. As the key step of their synthesis the Sonogashira cross-coupling reaction was successfully applied. The replacement of the C-O moiety by the C-C bond resulted in the loss of biological activity.

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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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34

Andrade, Valquiria, Mateus Mittersteiner, Helio Bonacorso, Clarissa Frizzo, Marcos Martins та Nilo Zanatta. "Regioselective Synthesis of 5-(Trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidines from β-Enamino Diketones". Synthesis 51, № 11 (2019): 2311–17. http://dx.doi.org/10.1055/s-0037-1611765.

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The use of β-enamino diketones as an easy entry to the regioselective synthesis of [1,2,4]triazolo[1,5-a]pyrimidines is reported. These ketones reacted with 3-amino-1H-1,2,4-triazoles to furnish exclusively 6-substituted 5-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidines in yields of up to 95%. The regioselectivity of the reactions performed was maintained regardless of the substituent in the starting ketone or aminoazole.

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35

Kathrotiya, Haresh G., and Yogesh T. Naliapara. "Synthesis of Novel Highly Substituted Pyrimidines Bearing Furanyl Thiazole Nucleous." International Letters of Chemistry, Physics and Astronomy 60 (September 2015): 47–57. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.60.47.

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A series of novel highly substituted pyrimidines bearing furanyl thiazole nucleous have been synthesized. In which reaction of guanidine nitrate with ketene dithioacetals 3c produced substituted pyrimidines 4d which further treated with various aromatic aldehydes to afford title compounds 5(a-t). The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.

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36

Kathrotiya, Haresh G., and Yogesh T. Naliapara. "Synthesis of Novel Highly Substituted Pyrimidines Bearing Furanyl Thiazole Nucleous." International Letters of Chemistry, Physics and Astronomy 60 (September 30, 2015): 47–57. http://dx.doi.org/10.56431/p-0c50ea.

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A series of novel highly substituted pyrimidines bearing furanyl thiazole nucleous have been synthesized. In which reaction of guanidine nitrate with ketene dithioacetals 3c produced substituted pyrimidines 4d which further treated with various aromatic aldehydes to afford title compounds 5(a-t). The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.

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37

Borzenko, Berta, Elena Bakurova, and Ksenia Mironova. "Disorders of purines and pyrimidines metabolism in human gastrointestinal tract cancer." Current Issues in Pharmacy and Medical Sciences 26, no. 4 (2013): 369–71. http://dx.doi.org/10.12923/j.2084-980x/26.4/a.02.

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38

Gomha, Sobhi, Ikhlass Abbas, Mohamed Elneairy, Mahmoud Elaasser, and Bazada Mabrouk. "Antimicrobial and anticancer evaluation of a novel synthetic tetracyclic system obtained by Dimroth rearrangement." Journal of the Serbian Chemical Society 80, no. 10 (2015): 1251–64. http://dx.doi.org/10.2298/jsc141222022g.

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A series of pyrido[3',2':4,5]thieno[2,3-e][1,2,4]triazolo[4,3-c]pyrimidines were prepared via oxidative cyclization of 4-(2-arylidenehydrazinyl)pyrido [3',2':4,5]thieno[3,2-d] pyrimidines. Dimroth rearrangement of such a series yielded pyrido[3',2':4,5]thieno[2,3-e][1,2,4]triazolo[1,5-c]pyrimidines. The reaction mechanism was proposed and the products were screened for their antimicrobial and anticancer activities. From the antimicrobial screening results, it can be seen that compounds 8c, 9f and 10c showed excellent activity against gram positive bacteria while compounds 10d and 8c showed the

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39

Abbas, Muhammad Akhtar, Fatima Batool, Iqra Ahmad Malik, Muzamil Haider, Habib Ullah Khan, and Mominul Islam Islam. "Synthesis and Characterization of Novel Fluorinated Pyrimidine Heterocyclic Derivatives as Pharmaceutical Agents." Journal of Pharma and Drug Regulatory Affairs 6, no. 2 (2024): 22–34. https://doi.org/10.46610/jpdra.2024.v06i02.003.

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Fluorinated pyrimidine derivatives represent a broad class of compounds that have received much attention owing to their wide range of applications such as pharmaceutical agents, anti-cancer, antimicrobial, antidepressant, antioxidant, antidiabetic, antiviral, antifungal, anti-herpes, and anti-tumor agents. Due to these pharmaceutical applications associated with fluorinated pyrimidines, we decided to synthesize them. Fluorinated pyrimidines have been synthesized via a one-pot multicomponent approach. All synthesized have been purified and characterized.

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40

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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41

A-Ani, Zaid S. M., Sana A. Abdulmawjood, Adel O. A. Al-Hussain, and Shihab A. Al-Bajari. "Synthesis and Biological Activity of few Pyrimidines Derivatives against Hepatic Injury Stimulated by Carbon Tetrachloride in Male Rats." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 12, no. 04 (2022): 1496–501. http://dx.doi.org/10.25258/ijddt.12.4.02.

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In the presence of sodium hydroxide, substituted chalcones are reacted with cyanoguandine in ethanol, and some chalcone compounds are used as a nucleus in the preparation of some five-, hexa-, and hepta-, heterocyclic compounds pyrimidine (pyrimidines derivatives), pyrimidine derivatives (A1, A2, and A3). Contains therapeutic properties and bioactivity, and has been used to treat various ailments. This study aimed to learn more about how pyrimidine derivatives could help mitigate the undesirable implications of carbon tetrachloride. a group of 50 male rats were separated into 5 groups: healthy

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42

Kassium, Yacoob Abdulla, and Khlood Abdulla Ahmed Hussein. "Synthesis and characterization of some new heterocyclic compounds with two Heteroatom's (Nitrogen) in their cyclic." University of Aden Journal of Natural and Applied Sciences 23, no. 2 (2019): 355–74. http://dx.doi.org/10.47372/uajnas.2019.n2.a08.

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The Pyrimidines derivatives play an essential role in several biological processes and have considerable important compounds for pharmaceutical medicinal and industrial material applications. The work describes the synthesis and characterization of some new pyrimidines derivatives: 2- mercapto 3,4 di hydro -4-oxo -[6- (4- alkoxy phenyl)- 4H)] pyrimidine -5- carbonitriles and 2- mercapto 3,4 di hydro -4-oxo -[6-(-4- substituted benzene - 4-H] pyrimidines -5- carbonitriles (3a-d). These Compounds (3a-d) were prepared from the reaction between ethylcyano acetate (0.01mole) and numbers of substitu

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43

Nwachukwu, Chideraa I., Leanna J. Patton, Nathan P. Bowling, and Eric Bosch. "Ditopic halogen bonding with bipyrimidines and activated pyrimidines." Acta Crystallographica Section C Structural Chemistry 76, no. 5 (2020): 458–67. http://dx.doi.org/10.1107/s2053229620005082.

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The potential of pyrimidines to serve as ditopic halogen-bond acceptors is explored. The halogen-bonded cocrystals formed from solutions of either 5,5′-bipyrimidine (C8H6N4) or 1,2-bis(pyrimidin-5-yl)ethyne (C10H6N4) and 2 molar equivalents of 1,3-diiodotetrafluorobenzene (C6F4I2) have a 1:1 composition. Each pyrimidine moiety acts as a single halogen-bond acceptor and the bipyrimidines act as ditopic halogen-bond acceptors. In contrast, the activated pyrimidines 2- and 5-{[4-(dimethylamino)phenyl]ethynyl}pyrimidine (C14H13N3) are ditopic halogen-bond acceptors, and 1:1 halogen-bonded cocrysta

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44

S., EL-BAHAIB, and G. ASSY M. "Synthesis and Biological Activity of some New Pyrimidines." J. Indian Chem. Soc. Vol. 66, Jul 1989 (1989): 463–64. https://doi.org/10.5281/zenodo.5996500.

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Department of Chemistry, Faculty of Science, Zagazig University, A. R. E. <em>Manuscript received 10 November 1988, accepted 23 May 1989</em> 4-Mercapto-6-methyl-2-(1-naphthyl)-5-acetylpyrlmldine (3) has been synthesised via the condensation of 1-naphthoyl isothiocyanate (1) with enaminone (2). The syntheses of isothiazolopyrimidine, pyrazolopyrimidine and 4-substituted-pyrimidines are also described. ·

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45

C., S. ANDOTR, KHAJURIA JATINDER, B. SINGH G., and SINGH SURJEET. "Synthesis and Biocidal Activity of some Substituted Pyrazolines and Pyrimidines." Journal of Indian Chemical Society Vol. 70, Mar 1993 (1993): 266–67. https://doi.org/10.5281/zenodo.6071901.

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Department of Chemistry, University of Jammu, Jammu-180 001 Department of Pharmacology, Regional Research Laboratory, Jammu <em>Manuscript received 24 August 1992, revised 18 December 1992, accepted 7 January 1993</em> Synthesis and Biocidal Activity of some Substituted Pyrazolines and Pyrimidines

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46

RAJEEV, JAIN, and SHIKHA GUPTA DEEPTI. "Synthesis of some New Arylazopyrazoles and Arylazopyrimidines." Journal of Indian Chemical Society Vol. 67, June 1990 (1990): 516–18. https://doi.org/10.5281/zenodo.6203998.

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School of Studies in Chemistry, Jiwaji University, Gwalior-474 011 <em>Manuscript received 11 September 1989, revised 24 January 1990, accepted 5 February 1990</em> Synthesis of some New Arylazopyrazoles and Arylazopyrimidines

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47

Delia, Thomas J., and Markus Baumann. "Fused pyrimidines.5. Methylated pyrimido[4,5-d]pyrimidines." Journal of Heterocyclic Chemistry 28, no. 6 (1991): 1553–56. http://dx.doi.org/10.1002/jhet.5570280615.

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48

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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49

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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50

Lin, Shu-Yu, Wen-Chieh Huang, Shwu-Chen Tsay, et al. "6-Chlorocoumarin Conjugates with Nucleobases and Nucleosides as Potent Anti-Hepatitis C Virus Agents." Molecules 30, no. 8 (2025): 1776. https://doi.org/10.3390/molecules30081776.

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On the basis of a “chemo-combination strategy”, (6-chloro)coumarin was incorporated to purines and pyrimidines, as well as their corresponding nucleosides, with a –SCH2– linker at different positions under alkaline conditions. These conjugates were found to exert an antiviral effect on the 1b subgenomic replicon replication of the hepatitis C virus (HCV) in Huh 5-2 and Huh 9-13 cells. In this compound library containing 14 new compounds, 6-[(6′-chlorocoumarin-3′-yl)methylthio]purine, 6-(6′-chlorocoumarin-3′-yl)methylthio-9-(β-D-ribofuranos-1″-yl)purine, and 2-[(6′-chlorocoumarin-3′-yl)methylth

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