Development of a scalable synthesis of a nonbasic inhibitor of the serine protease tryptase |
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| Authors: | Jeffrey M. Dener,Colin O&rsquo Bryan,Emma J. Shelton,Tania Mahajan,Jeffrey R. Spencer |
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| Affiliation: | a Department of Process Chemistry, Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, United States
b Department of Medicinal Chemistry, Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, United States |
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| 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. |
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