Irina O. Zhuravel

Solution-phase synthesis of a combinatorial library of 3-[4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides.

The parallel solution-phase synthesis of a new combinatorial library of 3-[4-(R1-coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides 9 has been developed. The synthesis involves two steps: 1) the synthesis of core building blocks – 3- [4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acids, 6 – by the reaction of 3-(ω-bromacetyl)coumarins 1 with 3-amino(thioxo)methylcarbamoylpropanoic acid (5); 2) the synthesis of the corresponding 3-[4-(coumarin-3-yl)-1,3-thiazol-2-yl- carbamoyl]propanoic acids amides 9 using 1,1’-carbonyldimidazole as a coupling reagent. The advantages of the method compared to existing ones are discussed.

Parallel Liquid-Phase Synthesis of 5-(1H-4-Pyrazolyl)-[1,2,4]oxadiazole Libraries

Combinatorial libraries of substituted 3-(methylthio)-5-(amino)-4-([1,2,4]oxadiazol-5-yl)-1H-pyrazoles 6, 10, 13, 15 (395 members, yields 32-87%), 4-([1,2,4]oxadiazol-5-yl)-1H-3,5-pyrazolediamines 8, 11 (571 members, yields 25-83%), 2-(methylthio)-3-([1,2,4]oxadiazol-5-yl)pyrazolo[1,5-a]pyrimidin-7(4H)-ones 17 (85 members, yields 56-95%), and 2-(amino)-3-([1,2,4]oxadiazol-5-yl)pyrazolo[1,5-a]pyrimidin-7(4H)-ones 18 (110 members, yields 56-95%) were synthesized by the parallel liquid-phase synthesis method.

Convenient Synthesis of Substituted 5‐(Hydroxymethyl)‐8‐methyl‐3‐(4‐phenylquinazolin‐2‐yl)‐2H‐pyrano[2,3‐c]pyridin‐2‐ones

Abstract Interaction of 2‐imino‐2H‐pyrano[2,3‐c]pyridin‐3‐carboxamide with substituted 2‐aminobenzophenones proceeds via recyclization mechanism leading to substituted 3‐(4‐arylquinazolyn‐2‐yl)‐2H‐pyrano[2,3‐c]pyridin‐2‐ones. Their reaction with acetic anhydride affords the O‐acylation products.

Synthesis of 5-Hydroxymethyl-8-methyl-3-(3-aryl-[1,2,4]oxadiazol-5-yl)-2H-pyrano[2,3-c]pyridin-2-ones and Their Esters

Abstract New 5-hydroxymethyl-8-methyl-3-(3-aryl-[1,2,4]oxadiazol-5-yl)-2H-pyrano-[2,3-c]pyridin-2-ones and their esters were synthesized. The structure of obtained compounds was determined through a complete 1H NMR analysis.

An Efficient Synthesis of 1,3,7-Triazaspiro[4.4]Nonane-2,4-Dione Derivatives and Antimicrobial Activity Thereof

Efficient methods for the synthesis of 1,3,7-triazaspiro[4.4]nonane-2,4-dione derivatives possessing an unsaturated pyrrolidine cycle have been developed affording intermediates and target compounds in high yields not requiring additional purification. Antimicrobial activity of the synthesized compounds was studied.