Selective -functionalization of Arylhydrazines with Primary Alcohols and Acids under PPh/DDQ System.

We present a PPh/DDQ-mediated regiospecific selective -functionalization of arylhydrazines with primary benzylic alcohols and aryl carboxylic acids for the synthesis of -benzyl arylhydrazines and -acyl arylhydrazines, respectively. This metal- and base-free approach features very short reaction times (about 10 min), broad substrate scope, good functional group tolerance, and mild reaction conditions. Furthermore, -benzlated products have also been successfully applied to the concise synthesis of -substituted indoles and anticancer drug MDM2 inhibitor.