Synthesis and biological evaluation of a phosphonate analog of the natural acetyl cholinesterase inhibitor cyclophostin

J Org Chem. 2008 Nov 7;73(21):8386-91. doi: 10.1021/jo801453v. Epub 2008 Sep 27.

Abstract

Two diastereomers of a phosphonate analog 6 of the AChE inhibitor cyclophostin were synthesized. The substitution reaction of phosphono allylic carbonate 10a with methyl acetoacetate gave the vinyl phosphonate 9a. Attempted hydrogenation/debenzylation gave an unexpected enolether lactone. Alternatively, selective hydrogenation, demethylation, cyclization and debenzylation gave the phosphonate analog of cyclophostin as a separable mixture of diastereomers 6. The trans phosphonate isomer was more active than the cis isomer against AChE from two sources.

Publication types

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

MeSH terms

  • Cholinesterase Inhibitors / chemistry*
  • Cyclization
  • Hydrogenation
  • Lactones
  • Organophosphonates / chemistry*
  • Organophosphorus Compounds / chemistry*
  • Structure-Activity Relationship

Substances

  • Cholinesterase Inhibitors
  • Lactones
  • Organophosphonates
  • Organophosphorus Compounds
  • cyclophostin