In the present invention, there is described an asymmetric synthesis process of a chiral compound of the general formula 6, in which P is an amino protecting group, by reacting a mixture of excess (lR,2S)-N-substituted norephedrine of the general formula 8 wherein R is C1-4 alkyl, or -NRi2 forms pyrrolidinyl or piperidinyl; with an excess of cyclopropylacetylene and an excess of a lithiating about with about one equivalent of the compound of the general formula 5 wherein P is as defined above, for improving synthesis process of an extremely active inhibitor of HIV reverse transcriptase, which inhibitor is (-)-6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, and the compound of the general formula 6, in which the P amino protecting group is selected from a group comprising: an alkyl group containing 1 to 4 carbon atoms, an optionally unsubstituted benzyl, 4-methoxybenzyl, 4-nitrobenzyl, 4-chlorobenzyl, 2,4-dichlorobenzyl, 2,4-dimethoxybenzyl, 4-methylsulfinylbenzyl, 9-anthrylmethyl, diphenylmethyl or N-trialkylsilyl.
展开▼
