Enantioselective Allylation of Stereogenic Nitrogen Centers

Org Lett. 2023 Mar 17;25(10):1649-1654. doi: 10.1021/acs.orglett.3c00195. Epub 2023 Mar 7.

Abstract

Most tertiary amines with a stereogenic nitrogen center undergo rapid racemization at room temperature. Consequently, the quaternization of amines under dynamic kinetic resolution seems feasible. N-Methyl tetrahydroisoquinolines are converted into configurationally stable ammonium ions by Pd-catalyzed allylic alkylation. The optimization of conditions and the evaluation of the substrate scope enabled high conversions and an enantiomeric ratio of up to 10:90. We report here the first examples for the enantioselective catalytic synthesis of chiral ammonium ions.