Total synthesis of (-)-laulimalide

J Am Chem Soc. 2002 May 8;124(18):4956-7. doi: 10.1021/ja0258428.

Abstract

(-)-Laulimalide (1), a structurally novel macrolide isolated in trace amounts from marine sponges, promotes abnormal tubulin polymerization and apoptosis in vitro, with a similar mode of action to that of Taxol(R), but with potentially less susceptibility to multidrug resistance. Herein, a flexible and convergent asymmetric synthesis of (-)-laulimalide is described. This synthesis featured a highly diastereoselective Sakurai reaction of 2 with 3 and a regioselective macrolactonization of an unprotected vicinal diol. Laulimalide was synthesized in 25 steps (longest linear; 36 overall) in 3.5% overall yield, providing a uniquely short and efficient route to 1 and its analogues.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Macrolides
  • Paclitaxel / analogs & derivatives*
  • Paclitaxel / chemical synthesis*
  • Stereoisomerism
  • Taxoids*

Substances

  • Antineoplastic Agents
  • Macrolides
  • Taxoids
  • laulimalide
  • Paclitaxel