Construction of α,β-Diamino Diacid Derivatives with Adjacent Acyclic Tetrasubstituted Stereocenters

J Org Chem. 2022 Jul 1;87(13):8709-8718. doi: 10.1021/acs.joc.2c00950. Epub 2022 Jun 17.

Abstract

A convenient strategy for the diastereoselective synthesis of α,β-diamino diacid derivatives bearing congested vicinal acyclic tetrasubstituted stereocenters via catalytic Mannich-type reactions of azlactones and 2-aminoacrylates was established. A diverse set of α,β-diamino diacid derivatives were synthesized in good to excellent yields and diastereoselectivities. Good enantioselectivity (up to 98:2 er) was achieved by employing the catalyst (DHQD)2PHAL in the subsequent asymmetric study.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Stereoisomerism*