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

Research output: Contribution to journal › Article › peer-review

DOI

https://doi.org/10.1007/s11172-014-0602-y
Final published version

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

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 language	English
Pages (from-to)	1350-1358
Number of pages	9
Journal	Russian Chemical Bulletin
Volume	63
Issue number	6
DOIs	https://doi.org/10.1007/s11172-014-0602-y
Publication status	Published - 1 Jan 2014

ASJC Scopus subject areas

Chemistry(all)

Research areas

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

WoS ResearchAreas Categories

Chemistry, Multidisciplinary

ID: 313581