Total synthesis of aplyronine C

Org Lett. 2013 Jun 21;15(12):3118-21. doi: 10.1021/ol401327r. Epub 2013 Jun 3.

Abstract

A highly stereocontrolled total synthesis of the cytotoxic marine macrolide aplyronine C is described. The route exploits aldol methodology to install the requisite stereochemistry and features a crucial boron-mediated aldol coupling of an N-vinylformamide-bearing methyl ketone with a macrocyclic aldehyde to introduce the full side chain. The synthesis of two novel C21-C34 side chain analogs is also reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Boron / chemistry
  • Macrolides / chemical synthesis*
  • Macrolides / chemistry
  • Molecular Structure
  • Stereoisomerism
  • Vinyl Compounds / chemistry*

Substances

  • Antineoplastic Agents
  • Macrolides
  • Vinyl Compounds
  • aplyronine C
  • Boron