Development of a scalable synthesis of a nonbasic inhibitor of the serine protease tryptase
JM Dener, C O'Bryan, R Yee, EJ Shelton, D Sperandio…
Index: Dener, Jeffrey M.; O'Bryan, Colin; Yee, Robert; Shelton, Emma J.; Sperandio, David; Mahajan, Tania; Palmer, James T.; Spencer, Jeffrey R.; Tong, Zhiwei Tetrahedron Letters, 2006 , vol. 47, # 27 p. 4591 - 4595
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Citation Number: 7
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 ...
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