Organocatalytic asymmetric allylic alkylation of 2-methyl-3-nitroindoles: a route to direct enantioselective functionalization of indole C(sp3)–H bonds

Abstract

We here described a direct catalytic asymmetric functionalization of 2-methylindoles using organocatalysis. An efficient asymmetric allylic alkylation reaction with respect to 2-methyl-3-nitroindoles and racemic Morita–Baylis–Hillman carbonate has been achieved by using a chiral biscinchona alkaloid catalyst, which provided the functionalized indole derivatives in good yields and enantioselectivities.