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 / Cheprakova E. M.,Verbitskiy E. V.,Ezhikova M. A.,Kodess M. I.,Pervova M. G.,Slepukhin P. A.,Toporova M. S.,Kravchenko M. A.,Medvinskiy I. D.,Rusinov G. L.,Charushin V. N. // RUSSIAN CHEMICAL BULLETIN. - 2014. - V. 63, l. 6. - P. 1350-1358.

ISSN/EISSN:
1066-5285 / 1573-9171
Type:
Article
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.
Author keywords:
pyrimidines; morpholine; thiomorpholine; cross-coupling; microwave irradiation; nucleophilic aromatic substitution of hydrogen; antituberculosis activity
DOI:
нет данных
Web of Science ID:
ISI:000350877500014
Соавторы в МНС:
Другие поля
Поле Значение
Month JUN
Publisher SPRINGER
Address 233 SPRING ST, NEW YORK, NY 10013 USA
Language English
EISSN 1573-9171
Research-Areas Chemistry
Web-of-Science-Categories Chemistry, Multidisciplinary
Author-Email Verbitsky@ios.uran.ru
Funding-Acknowledgement Ural Division of the Russian Academy of Sciences {[}12-P-3-1014, 12-T-3-1025, 12-T-3-1031, 13-3-019-UMA]; Russian Foundation for Basic Research {[}13-03-96049-p\_ural\_a, 13-03-90606-Arm\_a, 14-03-31040-mol\_a]; Council on Grants of the President of the Russian Federation {[}HSh-5505.2012.3, MK-3939.2014.3]; Ministry of Education and Science of RF {[}8430]; Government of the Sverdlovskaya region
Funding-Text This work was financially supported by the Ural Division of the Russian Academy of Sciences (Programs 12-P-3-1014, 12-T-3-1025, 12-T-3-1031, and 13-3-019-UMA), the Russian Foundation for Basic Research (Projects Nos 13-03-96049-p\_ural\_a, 13-03-90606-Arm\_a, and 14-03-31040-mol\_a), the Council on Grants of the President of the Russian Federation (Program for the State Support of the Leading Scientific Schools of RF, Grant HSh-5505.2012.3, and Program for the State Support of Young PhD-Scientists, Grant MK-3939.2014.3), Ministry of Education and Science of RF (Agreement No. 8430), and Government of the Sverdlovskaya region.
Number-of-Cited-References 11
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Journal-ISO Russ. Chem. Bull.
Doc-Delivery-Number CD2BC