Reaction of Bromoenones with Amidines: A Simple Catalyst-Free Approach to Trifluoromethylated Pyrimidines
Alexey R. Romanov, Alexander Yu. Rulev*, Alexander V. Popov, Evgeniy V. Kondrashov, Sergey V. Zinchenko
*A. E. Favorsky Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 1, Favorsky St., Irkutsk 664033, Russia,
Email: rulev
irioch.irk.ru
A. R. Romanov, A. Yu. Rulev, A. V. Popov, E. V. Kondrashov, S. V. Zinchenko, Synthesis, 2020, 52, 1512-1522.
DOI: 10.1055/s-0040-1707969
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Abstract
The reaction of trifluorinated 2-bromoenones with aryl- and alkylamidines provides trifluoromethylated pyrimidines in very good yields via an aza-Michael addition-intramolecular cyclization-dehydrohalogenation/dehydration cascade reaction. This strategy offers high selectivity and mild reaction conditions.
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Key Words
α-bromoenones, amidines, pyrimidines, aza-MIRC methodology, catalyst-free - mild conditions
ID: J66-Y2020
