Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type additions across α-chloro-N-sulfinylimines

Org Biomol Chem. 2012 Mar 21;10(11):2326-38. doi: 10.1039/c2ob06637h. Epub 2012 Feb 6.

Abstract

The efficient asymmetric synthesis of new chiral γ-chloro-α,β-diamino acid derivatives via highly diastereoselective Mannich-type reactions of N-(diphenylmethylene) glycine esters across a chiral α-chloro-N-p-toluenesulfinylimine was developed. The influence of the base, LDA or LiHMDS, used for the formation of the glycine enolates, was of great importance for the anti-/syn-diastereoselectivity of the Mannich-type reaction. The γ-chloro-α,β-diamino acid derivatives proved to be excellent building blocks for ring closure towards optically pure anti- and syn-β,γ-aziridino-α-amino esters, and subsequent ring transformation into trans-3-aminoazetidine-2-carboxylic acid derivatives and α,β-diamino-γ-butyrolactones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemistry*
  • Azetidines / chemistry*
  • Aziridines / chemistry*
  • Chlorine Compounds / chemistry*
  • Imines / chemistry*
  • Lactones / chemistry*
  • Models, Molecular
  • Molecular Structure
  • Stereoisomerism
  • Sulfur Compounds / chemistry*

Substances

  • Amino Acids
  • Azetidines
  • Aziridines
  • Chlorine Compounds
  • Imines
  • Lactones
  • Sulfur Compounds
  • azetidine
  • aziridine