Synthesis and Activity Evaluation of Gemcitabine Prodrugs with 4-(Boronic acid) benzoylamide Structure

Abstract A convenient approach was developed for the syntheses of amide derivatives and novel gemcitabine prodrugs with 4-(boronic acid) benzoylamide structure. The amide compounds containing the phenylboronic acid structure were synthesized by a one-step reaction strategy using o-toluidine and 4-boronobenzoic acid as starting materials. Also, the pure product was quickly obtained through acid–base post-treatment. Moreover, the prodrugs of gemcitabine containing phenylboronic acid structure were rapidly synthesized by the microchannel continuous flow technology. Three of all the obtained targets were subjected to the antiproliferative activity test.