Synthesis of N-BOH Benzazaborines via a Modular GBB-Based Strategy.

A green, one-pot Groebke-Blackburn-Bienaymé reaction is reported for the efficient synthesis of N-BOH benzazaborines. The products precipitate directly from methanol, enabling purification by simple filtration without chromatography. This scalable, operationally simple method uniquely combines synthetic efficiency with environmental sustainability, providing rapid access to boron-nitrogen scaffolds for medicinal chemistry.