European Journal of Organic Chemistry p. 5959 - 5961 (2011)
Update date:2022-08-04
Topics:
Kawai, Hiroyuki
Kitayama, Takashi
Tokunaga, Etsuko
Shibata, Norio
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. 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.
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