Atom-economic and stereoselective syntheses of the ring a and B subunits of the bryostatins

Chemistry. 2011 Aug 22;17(35):9777-88. doi: 10.1002/chem.201002930. Epub 2011 Jul 19.

Abstract

This article describes chemoselective and atom-economic methods for the stereoselective assembly of the ring A and B subunits of bryostatins. A Ru-catalyzed tandem alkene-alkyne coupling/Michael addition reaction was developed and applied to the synthesis of bryostatin ring B. We explored an acetylide-mediated epoxide-opening/6-exo-dig cyclization route to access the bryostatin ring A, although ring A was eventually furnished through an acid-catalyzed tandem transketalization/ketalization sequence. In addition, a dinuclear zinc-catalyzed methyl vinyl ketone (MVK) aldol strategy was evaluated for the construction of the polyacetate moiety. Utilization of these methods ultimately led to the rapid assembly of the northern bryostatin fragment containing both the ring A and B subunits.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Bryostatins / chemical synthesis*
  • Bryostatins / chemistry
  • Catalysis
  • Cyclization
  • Macrolides / chemical synthesis*
  • Macrolides / chemistry
  • Molecular Structure
  • Palladium / chemistry*
  • Stereoisomerism

Substances

  • Bryostatins
  • Macrolides
  • Palladium