Synthesis of 1,2-oxaborole via base-mediated borylation of propynols

Abstract

Boron-containing derivatives have numerous applications in medicinal, industrial, and synthetic chemistry. Considering this, a new, mild, catalyst-free, additive-free, base-assisted one-step robust method has been reported for the efficient synthesis of valuable 1,2-oxaborole derivatives via borylation of propynols using only cesium carbonate as a mild base. The reaction proceeds under mild conditions and demonstrates broad substrate scope and high functional group tolerance, making it suitable for a wide range of propargylic alcohols. Mechanistic investigations reveal that this method proceeds through a non-radical pathway.