Catalytic Enantioselective CH Borylation

Abstract

Abstract Organoboron compounds have proven to be versatile building blocks in the synthesis of natural products, organic materials, or drugs. The stereospecific transformations of optically active organoboron compounds, which represent an interesting class of enzyme inhibitors and have been used as marketed drugs themselves, potentially afford chiral products that are in growing demand for the screening of pharmaceutically active candidates. This amplifies the necessity to develop efficient and practical strategies to deliver enantioenriched organoboron compounds. Encouraged by this surging demand, an increasing number of racemic direct CH borylation reactions, which have been developed as a step and atom‐economic approach to borylated products, have evolved into their asymmetric versions based on elegantly designed chiral ligand and catalytic strategies. Herein, a brief summary of these breakthroughs is presented, especially emphasizing their connections with the racemic prototypical transformations. We expect that such introduction will inspire more efficient strategies in this field, enabling a more convenient access of chiral organoboron compounds.