E. V. Verbitskiy, S. A. Baskakova, D. V. Belyaev, D. V. Vakhrusheva, N. I. Eremeeva, G. L. Rusinov, V. N. Charushin, “Renaissance of 4-(5-nitrofuran-2-yl)-5-arylamino substituted pyrimidines: microwave-assisted synthesis and antitubercular activity”, Mendeleev Commun., 2021, Volume 31, Issue 2,Pages <nobr>210

This article is cited in 12 papers

Communications

Renaissance of 4-(5-nitrofuran-2-yl)-5-arylamino substituted pyrimidines: microwave-assisted synthesis and antitubercular activity

E. V. Verbitskiy^ab, S. A. Baskakova^a, D. V. Belyaev^ac, D. V. Vakhrusheva^c, N. I. Eremeeva^c, G. L. Rusinov^ab, V. N. Charushin^ab

^a I.Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Ekaterinburg, Russian Federation
^b Institute of Chemical Engineering, Ural Federal University, Ekaterinburg, Russian Federation
^c Ural Research Institute for Phthisiopulmonology, Ekaterinburg, Russian Federation

Abstract: The Buchwald–Hartwig cross-coupling of 5-bromo-4-(furan-2-yl)pyrimidine with various anilines afforded the corresponding new 5-(arylamino)pyrimidines, the reaction being accelerated by microwave irradiation. Most of the obtained compounds proved to possess a high bacteriostatic in vitro effect against Mycobacterium tuberculosis H₃₇Rv, Neisseria gonorrhoeae, and Staphylococcus aureus including Methicillin-resistant strain, which is stronger than that of the commercial drug Spectinomycin.

Keywords: pyrimidines, nitrofurans, anti-mycobacterial activity, Buchwald–Hartwig amination, cross-coupling reactions.

Language: English

DOI: 10.1016/j.mencom.2021.03.021

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