Iridium-Catalyzed Asymmetric Hydrogenation of gamma- and delta-Ketoacids for Enantioselective Synthesis of gamma- and delta-Lactones

摘要

A highly efficient asymmetric hydrogenation of gamma- and delta-ketoacids was developed by using a chiral Spiro iridium catalyst (S)-1a, affording the optically active gamma- and delta-hydroxy acids/lactones in high yields with excellent enantioselectivities (up to >99% ee) and turnover numbers (TON up to 100000). This protocol provides an efficient and practical method for enantioselective synthesis of Ezetimibe.