Cu–diamine ligand-controlled asymmetric Henry reactions and their application in concise total syntheses of linezolid and rivaroxaban

Abstract

A Cu-bis(sulfonamide)–diamine complex catalytic system was exploited in asymmetric Henry reactions to construct versatile chiral nitroalcohols with high enantioselectivity from carbamate-acetaldehydes and nitromethane. This elegant approach was further implemented to complete the asymmetric total syntheses of a series of oxazolidone skeleton drugs, such as linezolid (antibiotic) and rivaroxaban (anti-coagulant), in a concise and efficient way.