H3PO3/I2 mediated formation of N-benzyl benzo heterocyclic ketones from aromatic aldehydes and benzyl alcohol derivatives

Abstract

We report a H3PO3/I2 mediated formation of N-benzyl benzo heterocyclic ketones from the reaction of benzo heterocyclic compounds with aromatic aldehydes or benzyl alcohol derivatives under metal-free conditions in one-pot. For the first time, aromatic aldehydes were used as benzylated reagents to synthesize benzo heterocyclic ketones in the presence of K2CO3. Control experiments indicated that the carbonyl oxygen most possibly originated from K2CO3. H3PO3 also played the dual role of promotor as well as hydrogen source. This novel method features a wide substrate scope, low-cost and simple condition.