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A general strategy for the synthesis of difluoromethyl-containing pyrazoles, pyridines and pyrimidines |
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| Authors: | Viktor O. Iaroshenko Verena SpecowiusKatharina Vlach Marcelo Vilches-HerreraDmytro Ostrovskyi Satenik MkrtchyanAlexander Villinger Peter Langer |
| Affiliation: | a Institut für Chemie, Universität Rostock, Albert-Einstein-Str. 3a, 18059 Rostock, Germany b Department of Chemistry, National Taras Shevchenko University, 62 Volodymyrska st., Kyiv-33 01033, Ukraine c Leibniz-Institut für Katalyse an der Universität Rostock e.V., Albert Einstein Str. 29a, 18059 Rostock, Germany |
| Abstract: | Difluoromethyl-containing heteroannulated pyridines, pyrimidines and pyrazoles are prepared by a two step method. The regioselective cyclizations of electron-excessive aminoheterocycles, hydrazines and amidines with CF2Cl-substituted 1,3-dicarbonyl compounds provide the corresponding CF2Cl-substituted heterocycles. Subsequent radical reactions with trimethylstannane or allyltrimethylstannane gave difluoromethyl-containing heteroannulated pyridines, pyrimidines and pyrazoles, respectively. |
| Keywords: | Cyclizations Organofluorine compounds Regioselectivity Purine isosteres N-Heterocycles |
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