Toward tubulysin: gram-scale synthesis of tubuvaline-tubuphenylalanine fragment

J Org Chem. 2009 Dec 18;74(24):9531-4. doi: 10.1021/jo9015503.

Abstract

A practical and stereoselective synthesis of the tubuvaline-tubuphenylalanine (Tuv-Tup) fragment of tubulysin is achieved involving the opening of aziridine, crucial MacMillan alpha-hydroxylation on both fragments, and an epoxide-opening reaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acyclic Monoterpenes
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Aziridines / chemistry
  • Epoxy Compounds / chemistry
  • Hydroxylation
  • Monoterpenes / chemistry
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry*
  • Peptide Fragments / chemical synthesis*
  • Peptide Fragments / chemistry
  • Phenylalanine / chemical synthesis
  • Phenylalanine / chemistry*
  • Stereoisomerism
  • Valine / chemical synthesis
  • Valine / chemistry*

Substances

  • Acyclic Monoterpenes
  • Antineoplastic Agents
  • Aziridines
  • Epoxy Compounds
  • Monoterpenes
  • Oligopeptides
  • Peptide Fragments
  • tubulysin D
  • Phenylalanine
  • aziridine
  • Valine
  • citronellol