Straightforward synthesis of chiral non-racemic α-boryl isocyanides

Org Biomol Chem. 2021 Aug 5;19(30):6687-6691. doi: 10.1039/d1ob00616a.


A straightforward concise synthesis of chiral non-racemic aliphatic α-boryl isocyanides, relay intermediates for boron-based bioactive molecules in multicomponent reactions, is presented. The short synthetic sequence comprises as key steps copper-catalysed asymmetric borylation of imines, simultaneous nitrogen formylation/boron-protecting group interconversion and the final formamide dehydration reaction.

Publication types

  • Research Support, Non-U.S. Gov't