Asymmetric total synthesis of 1-deoxy-7,8-di-epi-castanospermine

Org Biomol Chem. 2010 Apr 7;8(7):1725-30. doi: 10.1039/b924721a. Epub 2010 Feb 9.

Abstract

An efficient, stereocontrolled synthesis of (6S,7S,8S,8aR)-6,7,8-trihydroxyindolizidine (alias 1-deoxy-7,8-di-epi-castanospermine) (14) has been developed, which exploits an asymmetric vinylogous Mukaiyama aldol reaction (VMAR) between N-(tert-butoxycarbonyl)-2-(tert-butyldimethylsilyloxy)pyrrole (1) and 2,3-O-isopropylidene-D-glyceraldehyde (2) to construct the initial pyrrolidine building block 3, and an ene-ene ring closing metathesis reaction (RCM) (9 to 10) to install the indolizidine skeleton. The synthetic sequence was 13 steps, proceeding in 19.5% overall yield. The configurational and conformational structure of 14 was ascertained unambiguously and confronted to previously published assignments of rac-14 and ent-14.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis*
  • Alkaloids / chemistry
  • Indolizines / chemical synthesis*
  • Indolizines / chemistry
  • Molecular Conformation
  • Stereoisomerism

Substances

  • Alkaloids
  • Indolizines
  • 1-deoxycastanospermine