Asymmetric Synthesis of Borylalkanes via Copper-Catalyzed Enantioselective Hydroallylation

J Am Chem Soc. 2016 Nov 23;138(46):15146-15149. doi: 10.1021/jacs.6b11229. Epub 2016 Nov 9.

Abstract

An efficient synthetic method for preparing enantioenriched secondary borylalkanes has been achieved through a copper-catalyzed regio- and enantioselective hydroallylation of alkenyl boronates and boramides employing hydrosilanes and allylic phosphates. In the presence of a copper catalyst with a chiral Walphos ligand, a range of alkenylboron compounds with an aryl, heteroaryl, or alkyl substituent produced secondary homoallylic alkylboron compounds in good yields and with high enantioselectivities up to 99% ee. The utility of the resulting alkylboronates was demonstrated in an efficient synthesis of (S)-massoialactone.

Publication types

  • Research Support, Non-U.S. Gov't