Rh-catalyzed asymmetric hydrogenation of allylic sulfones for synthesis of chiral β-ester sulfones

A general and highly efficient asymmetric hydrogenation of allylic sulfones catalyzed by the Rh-(R,R)-f-spiroPhos complex has been developed affording chiral beta-ester sulfones in high yields with excellent enantioselectivities (92-99.9% ee). The gram-scale hydrogenation was also successfully realized and this method can be used as an efficient concise synthetic route to key chiral intermediates of renin inhibitors: CGP 38 560 A and the macrocyclic renin inhibitors. The highly enantioselective hydrogenation of allylic sulfones catalyzed by Rh-(R,R)-f-spiroPhos for synthesis of chiral beta-ester sulfones has been developed for the first time achieving high yields and excellent enantioselectivities (92-99.9% ee).