Author/Authors :
Dener، نويسنده , , Jeffrey M. and O’Bryan، نويسنده , , Colin and Yee، نويسنده , , Robert D. Shelton ، نويسنده , , Emma J. and Sperandio، نويسنده , , David and Mahajan، نويسنده , , Tania and Palmer، نويسنده , , James T. and Spencer، نويسنده , , Jeffrey R. and Tong، نويسنده , , Zhiwei، نويسنده ,
Abstract :
A chromatography-free process for the synthesis of a bis(benzimidazole)difluoromethane inhibitor of the serine protease tryptase is described. This synthesis features the introduction of the gem-difluoro moiety using the electrophilic fluorinating reagent N-fluoro-bis(phenylsulfonimide) as well as the stepwise introduction of both benzimidazole rings. A protocol for the destruction of reactive, process-related substances produced in the synthesis is also presented.
