Total Syntheses of (+)-Gabosine P, (+)-Gabosine Q, (+)-Gabosine E, (-)-Gabosine G, (-)-Gabosine I, (-)-Gabosine K, (+)-Streptol, and (-)-Uvamalol A by a Diversity-Oriented Approach Featuring Tunable Deprotection Manipulation

J Org Chem. 2017 Apr 7;82(7):3692-3701. doi: 10.1021/acs.joc.7b00181. Epub 2017 Mar 20.

Abstract

A new diversity-oriented approach to C7-cyclitols, which possess a broad spectrum of biological activities, is developed. The key polyoxygenated intermediates with different O-protecting groups were accessed by an intramolecular aldol-cyclization of a diketone derived from δ-d-gluconolactone. The versatile intermediates can be easily transformed into structurally different carbasugars based on control of deprotection manipulation. The utility of the robust approach is illustrated by the first syntheses of (+)-gabosines P and Q, as well as the syntheses of several other gabosines and related analogues viz. (+)-gabosine E, (-)-gabosine G, (-)-gabosine I, (-)-gabosine K, (+)-streptol, and (-)-uvamalol A. In addition, the absolute configuration of (-)-uvamalol A is assigned by its total synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclization
  • Cyclohexanones / chemical synthesis*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Cyclohexanones