Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11beta-hydroxy steroid dehydrogenase type 1

摘要

The invention provides a process for preparing 11 beta-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.