Stereocontrolled total synthesis of amphidinolide X via a silicon-tethered metathesis reaction

Org Lett. 2008 Nov 20;10(22):5191-4. doi: 10.1021/ol8021676. Epub 2008 Oct 18.

Abstract

Two esterifications and an RCM to create the challenging trisubstituted C12-C13 double bond were required in the total synthesis of amphidinolide X (1) reported here. Assembling the three fragments in this order, no RCM occurred or the process yielded mainly isomer Z. However, generating the E double bond first, by a new variant of a Si-tethered metathesis (using Schrock's catalyst), and carrying out the esterification and macrolactonization steps later, 1 was obtained exclusively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Lactones / chemistry
  • Macrolides / chemical synthesis*
  • Macrolides / chemistry
  • Silicon / chemistry*
  • Stereoisomerism
  • Substrate Specificity

Substances

  • Lactones
  • Macrolides
  • amphidinolide X
  • Silicon