Catalytic Asymmetric Synthesis of Vicinal Tetrasubstituted Diamines via Umpolung Cross-Mannich Reaction of Cyclic Ketimines

Org Lett. 2020 Jul 2;22(13):5014-5019. doi: 10.1021/acs.orglett.0c01578. Epub 2020 Jun 22.

Abstract

A catalytic asymmetric umpolung cross-Mannich reaction of cyclic ketimines is realized. This protocol provides an efficient methodology for the facile synthesis of chiral vicinal tetrasubstituted diamines in high yields with excellent chemo-, regio-, diastereo-, and enantioselectivities using cinchona-derived bifunctional organocatalysts (85-98% yield, up to >20:1 dr, and >99% ee).

Publication types

  • Research Support, Non-U.S. Gov't