A convenient one-pot synthesis of benzoboroxoles has been developed via the reaction of o- bromobenzyl alcohols with NaH, nBuLi, and B (OiPr) 3 followed by acidic hydrolysis. Applications of these benzoboroxoles have been demonstrated in Pd-catalyzed cross- coupling reactions and the protocol has been extended for the synthesis of a chiral benzoboroxole. Exceptionally short synthesis of a potent antifungal agent AN2690 and ...