trans-Hydroboration of Propiolamides: Access to Primary and Secondary (E)-β-Borylacrylamides

Org Lett. 2019 Sep 6;21(17):6795-6799. doi: 10.1021/acs.orglett.9b02408. Epub 2019 Aug 8.

Abstract

A base-mediated trans-hydroboration of propiolamides that provides access to previously elusive primary and secondary (E)-β-borylacrylamide products has been developed. In the presence of n-butyllithium and pinacolborane, complete regioselectivity and stereoselectivity is observed, affording the corresponding vinylboronate products in up to 91% yield. A wide variety of primary and secondary amides served as efficient substrates for this transformation. A plausible reaction mechanism that involves substrate-assisted activation and a key intramolecular cyclization is discussed.

Publication types

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