NOVEL TWIN-DRUG TYPE C-2-SYMMETRICAL PHENYLBORONIC ACID PINACOL ESTERS

摘要

We here report the preparation of newly designed bivalent twin-drug type C-2-symmetrical cyclic phenylboronic acid derivatives. The synthesis of these C-2-symmetrical mid-size molecules 3 was accomplished by an amide bond formation reaction using amino-substituted phenylboronic acid pinacol esters 1 and dicarboxylic acid dichlorides 2 in the presence of Et3N. We confirmed that this procedure is conventionally applicable to the preparation of various C-2-symmetrical cyclic boronic acid derivatives 3 in good to excellent yields.