Asymmetric synthesis of the highly methylated tryptophan portion of the hemiasterlin tripeptides

Org Lett. 2002 Mar 7;4(5):695-7. doi: 10.1021/ol016982+.

Abstract

[reaction: see text] The asymmetric synthesis of the methylated tryptophan portion of hemiasterlin peptides is described. The key reactions are a SnCl4-mediated ring opening of epoxynitriles or epoxysulfones by N-methylindole followed by an asymmetric Strecker reaction. A second approach involving opening of glycidic esters by indoles is also described.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Methylation
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Porifera / chemistry
  • Stereoisomerism
  • Tryptophan / chemistry*

Substances

  • Antineoplastic Agents
  • Oligopeptides
  • hemiasterlin
  • Tryptophan