Synthesis of o-Methyl Trifluoromethyl Sulfide Substituted Benzophenones via 1,2-Difunctionalization of Aryne by Insertion into the C-C Bond.

ABSTRACT

An efficient process for the preparation of valuable o-methyl trifluoromethyl sulfide substituted benzophenones has been developed. The transition-metal-free method features insertion of aryne into a C-C σ-bond under mild reaction conditions for the first time to achieve ortho-difunctionalized arenes containing a pharmaceutically important trifluoromethylthio functional group. A wide substrate scope has been demonstrated for the developed protocol.