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Journal articles on the topic 'Pyrimidinols'

Author: Grafiati

Published: 4 June 2021

Last updated: 2 February 2022

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1

Valgimigli, Luca, Daniele Bartolomei, Riccardo Amorati, et al. "3-Pyridinols and 5-pyrimidinols: Tailor-made for use in synergistic radical-trapping co-antioxidant systems." Beilstein Journal of Organic Chemistry 9 (December 4, 2013): 2781–92. http://dx.doi.org/10.3762/bjoc.9.313.

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The incorporation of nitrogen atoms into the aromatic ring of phenolic compounds has enabled the development of some of the most potent radical-trapping antioxidants ever reported. These compounds, 3-pyridinols and 5-pyrimidinols, have stronger O–H bonds than equivalently substituted phenols, but possess similar reactivities toward autoxidation chain-carrying peroxyl radicals. These attributes suggest that 3-pyridinols and 5-pyrimidinols will be particularly effectiveco-antioxidants when used in combination with more common, but less reactive, phenolic antioxidants such as 2,6-di-tert-butyl-4-

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2

Wenska, Grazyna, Bohdan Skalski, and Zofia Gdaniec. "Transformation of 1-methyluracils and uridine to respective, 4-substituted pyrimdin-2(1H)-ones via pyridinium salts." Canadian Journal of Chemistry 70, no. 3 (1992): 856–62. http://dx.doi.org/10.1139/v92-113.

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1-Methyluracil and 1-methylthymine are converted into N-(1-methylpyrimidin-2-one-4-yl)- and N-(1-dimethylpyrimidin-2-one-4-yl)-pyridinium chlorides, respectively. The pyrimidinyl-pyridinium salts were then reacted with various nucleophiles under very mild conditions to give high yields of the desired 4-substituted pyrimidinones. In a similar manner 2′,3′,5′-tri-O-acetyluridine is efficiently converted into new 4-substituted pyrimidinone nucleosides.

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3

Adomėnienė, Ona, Povilas Adomėnas, Antanas Gleiznys, Aldona Beganskienė, Lidija Poloudina, and Yasuyuki Gotoh. "Mesomorphic Properties of New 5-Alkyl-2-Pyrimidinols Esters." Molecular Crystals and Liquid Crystals Science and Technology. Section A. Molecular Crystals and Liquid Crystals 364, no. 1 (2001): 739–43. http://dx.doi.org/10.1080/10587250108025043.

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4

Pratt, Derek A., Gino A. DiLabio, Giovanni Brigati, Gian Franco Pedulli, and Luca Valgimigli. "5-Pyrimidinols: Novel Chain-Breaking Antioxidants More Effective than Phenols." Journal of the American Chemical Society 123, no. 19 (2001): 4625–26. http://dx.doi.org/10.1021/ja005679l.

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5

Domínguez, Moisés, Matías Vidal, Macarena García-Arriagada, and Marcos Rezende. "Ultrasound-Promoted Synthesis of 4-Pyrimidinols and Their Tosyl Derivatives." Synthesis 48, no. 23 (2016): 4246–52. http://dx.doi.org/10.1055/s-0035-1562788.

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6

Wajon, J. F. M., та J. F. Arens. "The formation of pyrimidinols from α-acylbenzyl cyanides or α-acylphenylacetamides". Recueil des Travaux Chimiques des Pays-Bas 76, № 1 (2010): 79–91. http://dx.doi.org/10.1002/recl.19570760110.

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7

Nekkaa, Imane, Márta Palkó, István M. Mándity, and Ferenc Fülöp. "Continuous-flow retro-Diels–Alder reaction: an efficient method for the preparation of pyrimidinone derivatives." Beilstein Journal of Organic Chemistry 14 (February 1, 2018): 318–24. http://dx.doi.org/10.3762/bjoc.14.20.

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The syntheses of various pyrimidinones as potentially bioactive products by means of the highly controlled continuous-flow retro-Diels–Alder reaction of condensed pyrimidinone derivatives are presented. Noteworthy, the use of this approach allowed us to rapidly screen a selection of conditions and quickly confirm the viability of preparing the desired pyrimidinones in short reaction times. Yields typically higher than those published earlier using conventional batch or microwave processes were achieved.

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8

Latif, F. M. Abd El, A. S. Maghraby, M. A. Barsy, M. Z. A. Badr, and D. Dopp. "New Pyrazoline Derivatives." Collection of Czechoslovak Chemical Communications 59, no. 1 (1994): 247–52. http://dx.doi.org/10.1135/cccc19940247.

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The biological activity of azoles, pyrimidines as well as pyrazolines are of interest. Formation of pyrazolines and related compounds from hydrazine derivatives and α,β-unsaturated carbonyl compounds is very common. Pyrazoline fused with different heterocyclic nuclei at position 4 and 5 have been reported. Here we report the synthesis of some new monocyclic or fused azoles and pyrimidinones linked to C-4 or 5-chloro-3-methyl-1-phenylpyrazoline.

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9

Valgimigli, Luca, Giovanni Brigati, Gian Franco Pedulli, et al. "The Effect of Ring Nitrogen Atoms on the Homolytic Reactivity of Phenolic Compounds: Understanding the Radical-Scavenging Ability of 5-Pyrimidinols." Chemistry - A European Journal 9, no. 20 (2003): 4997–5010. http://dx.doi.org/10.1002/chem.200304960.

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10

Nielsen, P., and A. Bacher. "Biosynthesis of Riboflavin. A Simple Synthesis of the Substrate and Product of the Pyrimidine Deaminase and of Structural Analogs." Zeitschrift für Naturforschung B 43, no. 10 (1988): 1358–64. http://dx.doi.org/10.1515/znb-1988-1025.

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2-Amino-5-nitro-6-ribitylamino-4(3H)-pyrimidinone (7) was phosphorylated with chlorophosphoric acid yielding an isomer mixture containing about 63% of the 5´-phosphate 7a together with other monophosphates and bisphosphates of 7. Preparative HPLC afforded pure 7a. Catalytic hydrogenation of 7a yields the labile substrate of pyrimidine deaminase, 2,5-diamino-6-ribityl-amino-4(3H)-pyrimidinone 5´-phosphate (2a). The product of the enzyme, 5-amino-6-ribityl-amino-2,4(1H,3H)-pyrimidinedione 5´-phosphate (4a), can be obtained from 5-nitro-6-ribityl-amino-2,4(1H,3H)-pyrimidinedione (8) by an analogo

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11

Bhat, Sunita. "Synthesis and Antiviral Activity of Acyclic Nucleoside Analogues of 6-Methyluracil and 4-Alkylamino-6-methyl-2(1H)-pyrimidinones." Collection of Czechoslovak Chemical Communications 59, no. 3 (1994): 683–90. http://dx.doi.org/10.1135/cccc19940683.

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Reaction of 2,4-Dimethoxy-6-methylpyrimidine (I) with allyl bromide or benzyl bromide afforded 1-substituted 4-methoxy-6-methyl-2(1H)-pyrimidinone intermediates III, X. Oxidation of the compound III afforded racemic cis diol VI. O-Demethylation and nucleophilic displacement of the intermediates III, VI and X gave 1-substituted 6-methyluracils IV, VII, IX and 1-substituted 4-alkylamino-6-methyl-2(1H)-pyrimidinones V, VIII, XII in good yields. The compounds II - XII were evaluated against Ranikhet disease virus (RDV); compounds Vb, VII, X, XIIb - XIId showed 100, 43, 44, 75, 72 and 100% inhibiti

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12

Cheong, Siew Lee, Gopalakrishnan Venkatesan, Priyankar Paira, et al. "Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists: An Overview on the Structure-Activity Relationships." International Journal of Medicinal Chemistry 2011 (April 7, 2011): 1–15. http://dx.doi.org/10.1155/2011/480652.

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In the past few decades, medicinal chemistry research towards potent and selective antagonists of human adenosine receptors (namely, A1, A2A, A2B, and A3) has been evolving rapidly. These antagonists are deemed therapeutically beneficial in several pathological conditions including neurological and renal disorders, cancer, inflammation, and glaucoma. Up to this point, many classes of compounds have been successfully synthesized and identified as potent human adenosine receptor antagonists. In this paper, an overview of the structure-activity relationship (SAR) profiles of promising nonxanthine

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13

Kurth, Mark, Wonken Choung, Beth Lorsbach, Thomas Sparks, and James Ruiz. "4-(Isoxazol-3-yl)pyrimidines from Pyrimidinyl Nitrile Oxides." Synlett 2008, no. 19 (2008): 3036–40. http://dx.doi.org/10.1055/s-0028-1087346.

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14

Maddess, Matthew, and Rhiannon Carter. "SNAr Reactions of 2-Methylthio-4-pyrimidinones in Pivalic Acid: Access to Functionalized Pyrimidinones and Pyrimidines." Synthesis 44, no. 07 (2012): 1109–18. http://dx.doi.org/10.1055/s-0031-1289744.

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15

Bhaskar, Prakash, Suresha K. Tholappanavara, Bhuvanesh S. Kalal, et al. "Pyrimidinone Associated Triazole Carboxamides: Synthesis, Characterization, Cytotoxicity and DNA Binding Studies." Current Bioactive Compounds 16, no. 6 (2020): 911–23. http://dx.doi.org/10.2174/1573407215666190328222350.

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Background: Pyrimidinones and its derivatives are present in many anti-cancer agents. It has been reported that these substances were proven to have significant activities against different types of human cancers. The incorporation of [1,2,3]-triazole, a nitrogen-rich unit not only increases the efficacy but also increases the lipophilicity of the drug molecule. As our research was to synthesize newer molecules of effective cytotoxicity, we focused on pyrimidinone and [1,2,3]-triazoles systems, as important scaffolds with the expectation of potential cytotoxic properties. Methods: Novel series

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16

Maddess, Matthew L., and Rhiannon Carter. "ChemInform Abstract: SNAr Reactions of 2-Methylthio-4-pyrimidinones in Pivalic Acid: Access to Functionalized Pyrimidinones and Pyrimidines." ChemInform 43, no. 30 (2012): no. http://dx.doi.org/10.1002/chin.201230186.

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17

Fekri, Leila Z. "NiFe2O4@SiO2 @amino Glucose Magnetic Nanoparticle under Solvent-free Condition: A New, mild, Simple and Effective Avenue for the Synthesis of Quinazolinone, Imidazo[1,2-a]Pyrimidinone and Novel Derivatives of Amides." Current Organic Synthesis 17, no. 4 (2020): 304–12. http://dx.doi.org/10.2174/1570179417666200409151330.

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Background: Imidazo[1,2-a]pyrimidinone, quinazolinone and amide derivatives have attracted a lot of interest because of their broad scope of biological and pharmacological activities. There are a lot of methods reported in the literature for their synthesis. Therefore, we became interested in developing a convenient synthetic method for the preparation of imidazoquinazolinone and amide derivatives. Objective: NiFe2O4@SiO2 @glucose amine were synthesized, characterized and have been used for the green, effective and mild multicomponent synthesis of quinazolinones, benzoimidazo[1,2-a]pyrimidinon

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18

Botta, Maurizio, Francesco De Angelis, Gabriella Finizia, Rosario Nicoletti, and Maurizio Delfini. "6-alkyl- and 5,6-dialkyl-2-methoxy-4(3H)-pyrimidinones in the transformations of pyrimidines. Regiospecific 1--acylation of pyrimidines." Tetrahedron Letters 26, no. 28 (1985): 3345–48. http://dx.doi.org/10.1016/s0040-4039(00)98294-7.

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19

Nagaraj, Adki, and Cherkupally Sanjeeva Reddy. "Synthesis and biological study of novel methylene-bis-chalcones and substituted methylene-bis-pyrimidines/pyrimidinones." Journal of Heterocyclic Chemistry 44, no. 5 (2007): 1181–85. http://dx.doi.org/10.1002/jhet.5570440534.

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20

Falck-Pedersen, Mette Lene, Tore Benneche, Kjell Undheim, et al. "Palladium Catalysis in Allylic Rearrangements of Propenyl 2-Pyrimidinyl Carbonates to 1-Propenyl-2(1H)-pyrimidinones." Acta Chemica Scandinavica 47 (1993): 63–67. http://dx.doi.org/10.3891/acta.chem.scand.47-0063.

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21

Petricci, Elena, Claudia Mugnaini, Marco Radi, et al. "Towards new methodologies for the synthesis of biologically interesting 6-substituted pyrimidines and 4(3H)-pyrimidinones." Arkivoc 2006, no. 7 (2006): 452–78. http://dx.doi.org/10.3998/ark.5550190.0007.732.

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22

Fan, Junyuan, and C. C. Cheng. "Pyrimidines.24. Analogues and derivatives of 2-amino-5-bromo-6-phenyl-4(3H)-pyrimidinone (ABPP)." Journal of Heterocyclic Chemistry 30, no. 5 (1993): 1273–76. http://dx.doi.org/10.1002/jhet.5570300517.

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23

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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24

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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25

Sugimoto, Osamu, Ken-ichi Tanji, and Takeshi Yokoi. "The One-Pot Conversion of Pyrimidinone Derivatives into Substituted Pyrimidines Using Diphenylphosphinic Chloride under a Mild Condition." HETEROCYCLES 60, no. 2 (2003): 413. http://dx.doi.org/10.3987/com-02-9659.

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26

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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27

Wang, Hsiao-Fen, Kuang-Hway Yih та Gene-Hsiang Lee. "Syntheses, Reactivities, Characterization, and Crystal Structures of Dipalladium Complexes Containing the 1,3-pyrimidinyl Ligand: Structures of [Pd(PPh3)(Br)]2(μ,η2-C4H3N2)2, [Pd(Br)]2(μ,η2-Hdppa)2, and [{Pd(PPh3)(CH3CN)}2(μ,η2-C4H3N2)2][BF4]2". Molecules 25, № 9 (2020): 2035. http://dx.doi.org/10.3390/molecules25092035.

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In a refluxing chloroform solution, the η1-pyrimidinyl {pyrimidinyl = C4H3N2} palladium complex [Pd(PPh3)2(η1-C4H3N2)(Br)], 1 exhibited intermolecular displacement of two triphenylphosphine ligands to form the doubly bridged η2-pyrimidinyl Dipalladium complex [Pd(PPh3)(Br)]2(μ,η2-C4H3N2)2, 3. The treatment of 1 with Hdppa {Hdppa = N,N-bisdiphenyl phosphinoamine} in refluxing dichloromethane yielded the doubly bridged Hdppa dipalladium complex [Pd(Br)]2(μ,η2-Hdppa)2, 4. Complex 1 reacted with the bidentate ligand, NH4S2CNC4H8 and, NaS2COEt, and the tridentate ligand, KTp {Tp = tris(pyrazoyl-1-y

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28

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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29

Lee, Hyuck Joo, and Yang-Heon Song. "A facile one-pot synthesis of aryl-substituted fused pyrimidinones." Heterocyclic Communications 22, no. 2 (2016): 59–62. http://dx.doi.org/10.1515/hc-2015-0262.

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AbstractThe convenient synthesis of a series of 3-phenylpyrido[1,2-a]pyrimidinones 4, 3-phenylpyrimido[1,2-c]quinazolinones 7 and 3-phenylpyrazino[1,2-a]pyrimidinones 10 with promising biological activity is presented.

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30

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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31

FALCK-PEDERSEN, M. L., T. BENNECHE, and K. UNDHEIM. "ChemInform Abstract: Palladium Catalysis in Allylic Rearrangements of Propenyl 2- Pyrimidinyl Carbonates to 1-Propenyl-2(1H)-pyrimidinones." ChemInform 24, no. 20 (2010): no. http://dx.doi.org/10.1002/chin.199320230.

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32

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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33

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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34

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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35

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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36

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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37

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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38

Zou, Jian-Ping, Wei Zhang, Cheng-Kun Li, et al. "Mn(OAc)3-Mediated Regioselective Radical Alkoxycarbonylation of Indoles, Pyrimidinones, and Pyridinones." Synthesis 50, no. 15 (2018): 2968–73. http://dx.doi.org/10.1055/s-0037-1610039.

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Mn(OAc)3-mediated alkoxycarbonylation of indoles, pyrimidinones, and pyridinones with alkyl carbazates is reported. The reactions proceed through a radical process to afford regioselectively 3-carboxylated indoles, 5-carboxylated pyrimidinones, and 3-carboxylated pyridinones in moderate to good yields under mild reaction conditions.

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39

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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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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Murray, J. B., C. J. Adams, J. R. P. Arnold, and P. G. Stockley. "The roles of the conserved pyrimidine bases in hammerhead ribozyme catalysis: evidence for a magnesium ion-binding site." Biochemical Journal 311, no. 2 (1995): 487–94. http://dx.doi.org/10.1042/bj3110487.

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We report details of the synthesis and characterization of oligoribonucleotides containing 4-thiouridine or 2-pyrimidinone ribonucleoside (4HC). We have used these probes to examine the roles of the conserved pyrimidines in the central core of the hammerhead ribozyme. The effects on catalysis of singly-substituted hammerhead ribozyme and substrate strands were quantified in multiple-turnover reactions. Various effects were observed on kcat. and Km, with up to a 7-fold decrease and a 3-fold increase respectively. For substitutions with 4HC at positions 3 or 17, catalytic activity in single turn

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FAN, J., and C. C. CHENG. "ChemInform Abstract: Pyrimidines. Part 24. Analogues and Derivatives of 2-Amino-5-bromo-6- phenyl-4(3H)-pyrimidinone (ABPP)." ChemInform 25, no. 19 (2010): no. http://dx.doi.org/10.1002/chin.199419178.

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Shirsale, Ashwini, Yogesh Patil, Girish Rawal, et al. "A Convenient and Concise Metal-Free Approach to Functionalized Bicyclic Pyrimidinones from Oxazine-2,6-diones." Synthesis 50, no. 10 (2018): 2087–93. http://dx.doi.org/10.1055/s-0037-1609364.

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The synthesis of previously unreported pyrazolo-pyrimidinones and isoxazolo-pyrimidinones are achieved via metal-free coupling of oxazine-2,6-diones with pyrazolidinone and isoxazolidinone, respectively. The synthesis provides easy access to a variety of novel 2-dimensional building blocks that can be derivatized to generate a range of drug- and agro-like molecules.

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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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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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Zribi, Fethi, Mansour Salem, and Fakher Chabchoub. "Reactivity of Hydrazine, Some Hydrazine derivatives and Diamines toward Ethyl 2,2-Dicyano-1-aryl (or alkyl)vinylcarbamate." JOURNAL OF ADVANCES IN CHEMISTRY 10, no. 2 (2014): 2197–202. http://dx.doi.org/10.24297/jac.v10i2.979.

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A series of pyrimidinone and dipyrimidinone derivatives 2a-c, 4a-e and 6a-f has been synthesized via the reaction between ethyl 2,2-dicyano-1-aryl(or alkyl)vinylcarbamate derivatives 1a-d and hydrazine derivatives or diamines. The reactivity of compounds 1a-d toward hydrazine is studied. The result is the formation of triazolones 5a-d rather than pyrimidinone derivatives.

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Viramgama, Piyush. "Microwave assisted synthesis of 1,2,4-triazolo [1,5-a]pyrimidines and biological evaluation." International Journal of Scientific Research 1, no. 7 (2012): 8–10. http://dx.doi.org/10.15373/22778179/dec2012/4.

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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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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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Smicius, Romualdas, Virginija Jakubkiene, Milda M. Burbuliene, Aiste Mikalainyte, and Povilas Vainilavicius. "Synthesis of 1-(6-Methyl-2,4-Dioxo-1,2,3,4-Tetrahydro-3-Pyrimidinyl)Acetyl-4-Alkyl(Aryl)Thiosemicarbazides and their Heterocyclisation to 1,2,4-Triazoles and 1,3,4-Thiadiazoles." Journal of Chemical Research 2002, no. 4 (2002): 170–72. http://dx.doi.org/10.3184/030823402103171555.

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5-(6-Methyl-2,4-dioxo-1,2,3,4-tetrahydro-3-pyrimidinyl)methyl-1,3,4-oxadiazole-2-thione reacts with amines to give 1-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-3-pyrimidinyl)acetyl-4-alkyl(aryl)thiosemicarbazides, which on treatment with base or acid undergo cyclisation to 4-alkyl-1,2,4-triazole-2-thiones or 4-amino-1,3,4-thiadiazoles, respectively.

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