EFFICIENT METHOD FOR THE SYNTHESIS OF NOVEL SUBSTITUTED THIENO[2,3-d]PYRIMIDINE-4-CARBOXYLIC ACIDS, THEIR DERIVATIZATION, AND ANTIMICROBIAL ACTIVITY

Authors

  • Елена Д. Власова National University of Pharmacy
  • Константин Ю. Кроленко Enamine Ltd.
  • Максим А. Нечаев Enamine Ltd.
  • Павел Е. Шинкаренко Enamine Ltd.
  • Владимир И. Кабачный Национальный фармацевтический университет
  • Сергей В. Власов Национальный фармацевтический университет

DOI:

https://doi.org/10.1007/4864

Keywords:

amides, carboxylic acids, pyrimidine, thiophene, antibacterial activity, carbonylation.

Abstract

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.

Published

2019-03-12

Issue

Section

Original Papers