Exploiting pseudo C2-symmetry for an efficient synthesis of the F-ring of the spongistatins

Org Lett. 2013 Nov 1;15(21):5464-7. doi: 10.1021/ol402604s. Epub 2013 Oct 10.

Abstract

A concise and efficient synthesis of the F-ring fragment of the potent antimitotic marine macrolide spongistatin 1 has been developed. The key sequence involves double cross-metathesis/Sharpless asymmetric dihydroxylation reactions to establish four stereocenters in a pseudo C2-symmetric array, followed by a selective protection reaction that breaks the pseudosymmetry, establishes a fifth stereocenter, and effectively differentiates the ester termini. Overall, the six contiguous stereocenters in the C(37)-C(45) F-ring fragment are established in just seven steps.

Publication types

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

MeSH terms

  • Macrolides / chemical synthesis*
  • Macrolides / chemistry
  • Molecular Structure
  • Stereoisomerism

Substances

  • Macrolides
  • spongistatin 1