A convergent process for the preparation of adamantane 11-β-HSD-1 inhibitors

CL Becker, KM Engstrom, FA Kerdesky…

Index: Becker, Calvin L.; Engstrom, Kenneth M.; Kerdesky, Francis A.; Tolle, John C.; Wagaw, Seble H.; Wang, Weifeng Organic Process Research and Development, 2008 , vol. 12, # 6 p. 1114 - 1118

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Citation Number: 13

Abstract

A convergent, scalable process was developed for the synthesis of adamantane 11-β- hydroxysteroid dehydrogenase-1 inhibitors E-4-(2-methyl-2-(4-(5-(trifluoromethyl) pyridin-2- yl) piperazin-1-yl) propionylamino) adamantane-1-carboxylic acid (1) and E-4-(2-methyl-2-(4- (5-(trifluoromethyl) pyridin-2-yl) piperazin-1-yl) propionylamino) adamantane-1-carboxamide (2) to rapidly deliver material for development. The process was high yielding and ...