New stereodivergent approach to 3-amino-2,3,6-trideoxysugars. Enantioselective synthesis of daunosamine, ristosamine, acosamine, and epi-daunosamine

Org Lett. 2003 Aug 21;5(17):3001-4. doi: 10.1021/ol034843h.

Abstract

[reaction: see text] An enantioselective preparation of the four diastereomeric 3-amino-2,3,6-trideoxy-hexoses, key components of anthracycline antibiotics, has been developed. Sharpless catalytic asymmetric epoxidation of the (2E)-2,5-hexadien-1-ol, regioselective ring opening with azide, followed by convenient functional group transformations, afforded the key aldehydes cis- or trans-6 in any configuration. The diastereoselective addition of methylmetal reagents to these aldehydes followed by ozonolysis gives access in a completely stereocontrolled manner to the four isomeric trideoxyaminosugars.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry
  • Azides / chemistry
  • Carbohydrate Conformation
  • Hexosamines / chemical synthesis*
  • Hexosamines / chemistry
  • Methylation
  • Ozone / chemistry
  • Stereoisomerism

Substances

  • Aldehydes
  • Azides
  • Hexosamines
  • daunosamine
  • ristosamine
  • acosamine
  • Ozone