The stereocontrolled total synthesis of altohyrtin A/spongistatin 1: the CD-spiroacetal segment

Org Biomol Chem. 2005 Jul 7;3(13):2410-9. doi: 10.1039/b504148a. Epub 2005 May 24.

Abstract

Stereocontrolled syntheses of the C16-C28 CD-spiroacetal subunit of altohyrtin A/spongistatin 1 , relying on kinetic and thermodynamic control of the spiroacetal formation, are described. The kinetic control approach resulted in a slight preference (60 : 40) for the desired spiroacetal isomer. The thermodynamic approach allowed ready access to the desired spiroacetal by acid-promoted equilibration, chromatographic separation of the C23 epimers and resubjection of the undesired isomer to the equilibration conditions. This scalable synthetic sequence provided multi-gram quantities of , thus enabling the successful completion of the total synthesis of altohyrtin A/spongistatin 1, as reported in Part 4 of this series.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetals / chemical synthesis
  • Antineoplastic Agents / chemical synthesis*
  • Kinetics
  • Macrolides / chemical synthesis*
  • Molecular Structure
  • Spiro Compounds / chemical synthesis
  • Stereoisomerism
  • Thermodynamics

Substances

  • Acetals
  • Antineoplastic Agents
  • Macrolides
  • Spiro Compounds
  • spongistatin 1