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Efficient method for the synthesis of novel substituted thieno[2,3-d]pyrimidine-4-carboxylic acids, their derivatization, and antimicrobial activity

Chem. Heterocycl. Compd. 2019, 55 (2), 184-188

DOI: 10.1007/s10593-019-02437-1

Vlasova O.; Krolenko K.; Nechayev M.; Shynkarenko P.; Kabachnyy V.; Vlasov S.

An effective method for accessing novel substituted thieno[2,3-d]pyrimidine-4-carboxylic acids in 63–71% yields based on Pd(dppf)Cl2-catalyzed carbonylation of substituted 4-chlorothieno[2,3-d]pyrimidines has been proposed; a procedure has been developed for obtaining the amides of these acids, suitable for liquid-phase combinatorial synthesis, in 53–77% yields. Compounds with antimicrobial activity against Pseudomonas aeruginosa similar to the reference drug streptomycin were found among the synthesized amides.

Efficient method for the synthesis of novel substituted thieno[2,3-d]pyrimidine-4-carboxylic acids, their derivatization, and antimicrobial activity

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