EFFICIENT ENANTIOSELECTIVE ADDITION REACTION USING AN ORGANOZINC REAGENT

摘要

An efficient method for the preparation of key intermediate, in the synthesi s of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2- trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.