Litcius/Paper detail

Iridium-Catalyzed Enantioselective Direct α-C–H Alkylation of Saturated Cyclic Amines with Alkenes

Daisuke Yamauchi, Kentaro Yamakawa, Takahiro Nishimura

2022Organic Letters14 citationsDOI

Abstract

Enantioselective direct α-C(sp3)–H alkylation of saturated cyclic amines having N-methylbenzimidazolyl as a directing group was realized by using a cationic iridium/chiral diphosphine catalyst. The alkylation of pyrrolidine derivatives with various terminal alkenes proceeded to give α-alkylated products in high yields with high enantioselectivities. Chiral α,α′-dialkylated pyrrolidine derivatives were also synthesized by using an excess of alkenes or by stepwise alkylation.

Topics & Concepts

AlkylationChemistryPyrrolidineEnantioselective synthesisIridiumCatalysisCationic polymerizationOrganic chemistryMedicinal chemistryCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsAsymmetric Hydrogenation and Catalysis