Convenient asymmetric synthesis of beta-trifluoromethyl-beta-amino acid, beta-amino ketones, and gamma-amino alcohols via Reformatsky and Mannich-type reactions from 2-trifluoromethyl-1,3-oxazolidines

J Org Chem. 2006 Mar 3;71(5):2159-62. doi: 10.1021/jo052323p.

Abstract

The stereoselective syntheses of beta-trifluoromethyl-beta-amino ester, beta lactams, and beta-amino ketones starting from an oxazolidine derived from trifluoroacetaldehyde hemiacetal and (R)-phenylglycinol are reported. The Mannich-type reaction involving a chiral fluorinated iminium ion occurred in a good yield and with a higher stereoselectivity (dr up to 96:4) than that of the Reformatsky-type reaction. This straightforward strategy was applied to the short syntheses of (R)-3-amino-4,4,4-trifluorobutanoic acid, a series of novel enantiopure unprotected fluorinated beta-amino ketones, and their corresponding gamma-amino alcohols.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemical synthesis*
  • Amino Alcohols / chemical synthesis*
  • Ketones / chemical synthesis*
  • Oxazoles / chemistry*
  • Stereoisomerism

Substances

  • Amino Acids
  • Amino Alcohols
  • Ketones
  • Oxazoles