Solid-phase organic synthesis of difluoroalkyl entities using a novel fluorinating cleavage strategy: part 2. Synthesis of three small gem-difluorinated compound libraries using a dithiane linker

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.