Synthesis of 5-(het)aryl- and 4,5-di(het)ary1-2-(thio)morpholinopyrimidines from 2-chloropyrimidine via S-N(H) and cross-coupling reactions

E. M. Cheprakova, E. V. Verbitskiy, M. A. Ezhikova, M. I. Kodess, M. G. Pervova, P. A. Slepukhin, M. S. Toporova, M. A. Kravchenko, I. D. Medvinskiy, G. L. Rusinov, V. N. Charushin

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

It has been shown that various combinations of nucleophilic aromatic substitution of hydrogen (S-N(H)), S-N(ipso) and the microwave-assisted Suzuki cross-coupling reactions are a versatile method for the synthesis of 5-(het)ary1-2-(thio)morpholinopyrimidine and 4,5-di(het)ary1-2(thio)morpholinopyrimidine derivatives. All synthesized pyrimidines were found to be active in micromolar concentrations in vitro against Mycobacterium tuberculosis H(37)Rv.
Original languageEnglish
Pages (from-to)1350-1358
Number of pages9
JournalRussian Chemical Bulletin
Volume63
Issue number6
DOIs
Publication statusPublished - 1 Jan 2014

Keywords

  • antituberculosis activity
  • cross-coupling
  • microwave irradiation
  • morpholine
  • nucleophilic aromatic substitution of hydrogen
  • pyrimidines
  • thiomorpholine

ASJC Scopus subject areas

  • Chemistry(all)

WoS ResearchAreas Categories

  • Chemistry, Multidisciplinary

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