An efficient and facile synthesis of deuterium-labeled anticancer agent bendamustine hydrochloride

摘要

Bendamustine hydrochloride is an alkylating agent that was developed for the treatment of various human cancers. The stable isotope-labeled bendamustine was required to support clinic studies. An effective and operationally simple method for the synthesis of [D-6] bendamustine hydrochloride was developed using DCl as a catalyst and D2O as a deuterium source. Under the present condition, regioselectively deuterated bendamustine hydrochloride with high deuterium incorporation is achieved.