Stereospecific Coupling of Boronic Esters with N-Heteroaromatic Compounds

J Am Chem Soc. 2015 Sep 2;137(34):10958-61. doi: 10.1021/jacs.5b07842. Epub 2015 Aug 21.

Abstract

A protocol for the stereospecific coupling of chiral secondary and tertiary boronic esters with lithiated N-heteroaromatics is described. The process involves initial boronate complex formation followed by addition of Troc-Cl, which activates the nitrogen and induces 1,2-migration. Oxidative workup furnishes the coupled product with >98% es.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boronic Acids / chemistry*
  • Esters / chemistry*
  • Heterocyclic Compounds / chemistry*
  • Hydrocarbons, Aromatic / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Boronic Acids
  • Esters
  • Heterocyclic Compounds
  • Hydrocarbons, Aromatic