Asymmetric synthesis of alpha,alpha-dibranched propargylamines by acetylide additions to N-tert-butanesulfinyl ketimines

J Org Chem. 2006 Sep 1;71(18):7110-2. doi: 10.1021/jo061160h.

Abstract

Addition of lithium acetylides prepared from 1-pentyne, phenylacetylene, and trimethylsilylacetylene to diverse N-tert-butanesulfinyl ketimines affords a range of alpha,alpha-dibranched propargyl sulfinamides in generally good yields (up to 87%) and with high diastereoselectivities (up to >99:1). Acidic cleavage of the tert-butanesulfinyl group provides the free alpha,alpha-dibranched propargylamines.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Chemistry, Organic / methods*
  • Pargyline / analogs & derivatives*
  • Pargyline / chemical synthesis
  • Pargyline / chemistry
  • Propylamines / chemical synthesis
  • Propylamines / chemistry*
  • Stereoisomerism
  • Sulfonium Compounds / chemistry

Substances

  • Propylamines
  • Sulfonium Compounds
  • propargylamine
  • Pargyline