Solid-phase organic synthesis of difluoroalkyl entities using a novel fluorinating cleavage strategy: part 2.
Matthias S Wiehn1, Daniel Fürniss, Stefan Bräse
1Institut fur Organische Chemie, Karlsruhe Institute of Technology, Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany.
Abstract:
Three small compound biaryl libraries featuring a novel fluorinating cleavage strategy for preparation of a difluoromethyl group were assembled on solid supports. The average reaction yield per step was up to 96% in a synthetic sequence over five to six steps. Key features were Suzuki coupling reactions, transesterification with potassium cyanide and amidation reaction with trimethyl aluminum on solid supports.
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