Abstract 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.
