Aryl Borane as a Catalyst for Dehydrative Amide Synthesis

Abstract

Tris(pentafluorophenyl)borane B(C₆F₅)₃·H₂O is reported as a catalyst for dehydrative amidation of carboxylic acids and amines. This protocol is applicable across a wide range of >35 substrates, including aromatic and aliphatic amines and acids, resulting in amides in ≤92% yields. The scalability of the reaction up to 10 mmol, along with the synthesis of drugs such as ibuprofen amide, moclobemide, and phenacetin, demonstrates the industrial potential of our protocol.