A New Synthetic Approach to Efavirenz through Enantioselective Trifluoromethylation by Using the Ruppert-Prakash Reagent

The organocatalyzed asymmetric synthesis of efavirenz was achieved in five steps from a commercially available substrate through the operationally simple, enantioselective trifluoromethylation of an alkynyl ketone by using the Ruppert-Prakash reagent. The present method provides the first example of the enantioselective synthesis of efavirenz by using a direct trifluoromethylation approach.