(+)-Rimocidin synthetic studies: construction of the C(1-27) aglycone skeleton

J Org Chem. 2009 Aug 21;74(16):5987-6001. doi: 10.1021/jo900765p.

Abstract

Assembly of the C(1-27) macrocyclic skeleton of rimocidinolide, the aglycone of (+)-rimocidin (1), has been achieved in convergent fashion. Key features of the synthetic strategy entail application of multicomponent Type I Anion Relay Chemistry (ARC), in conjunction with the S(N)2/S(N)2' reaction manifolds of vinyl epoxides, both employing 2-substituted 1,3-dithianes to construct the C(1-19) carbon backbone. Yamaguchi union of a C(20-27) vinyl borate ester, possessing the all-trans triene, with an advanced C(1-19) vinyl iodide followed by macrocyclization via Suzuki-Miyaura cross-coupling completed construction of the C(1-27) rimocidinolide skeleton.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Borates / chemistry
  • Carboxylic Acids / chemistry
  • Epoxy Compounds / chemistry
  • Macrocyclic Compounds / chemistry*
  • Polyenes / chemical synthesis
  • Polyenes / chemistry
  • Pyrans / chemistry
  • Quinolizines / chemistry
  • Stereoisomerism
  • Sulfur Compounds / chemistry

Substances

  • Borates
  • Carboxylic Acids
  • Epoxy Compounds
  • Macrocyclic Compounds
  • Polyenes
  • Pyrans
  • Quinolizines
  • Sulfur Compounds
  • dithiane
  • rimocidin