Synthesis of Benzyl-, Allyl-, and Allenyl-boronates via Copper-Catalyzed Borylation of Alcohols

Org Lett. 2017 Mar 3;19(5):1204-1207. doi: 10.1021/acs.orglett.7b00256. Epub 2017 Feb 16.

Abstract

Alcohols are among the most abundant and readily available organic feedstocks in industrial processes. The direct catalytic functionalization of sp3 C-O bonds of alcohols remains the main challenge in this field. Here, we report a copper-catalyzed synthesis of benzyl-, allyl-, and allenyl-boronates from benzylic, allylic, and propargylic alcohols, respectively. This protocol exhibits a broad reaction scope (40 examples) and high efficiency (up to 95% yield) under mild conditions, including for the preparation of secondary allylic boronates. Preliminarily mechanistic studies suggest that nucleophilic substitution is involved in this reaction.

Publication types

  • Research Support, Non-U.S. Gov't