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רÀûºÅ        CN101786959
ÉêÇëºÅ        CN200910045985.9
רÀûºÅÉêÇëÈÕÆÚ        2009.01.23
¹«¿ªÈÕÆÚ        2010.07.28
Ö÷·ÖÀàºÅ        C07C215/68(2006.01)I
·ÖÀàºÅ         C07C215/68(2006.01)I;C07C213/00(2006.01)I;C07C213/10(2006.01)I;C07B53/00(2006.01)I
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The invention relates to the method for synthesizing chiral cyclopropyl ethynyl tert-alc. deriv., (S)-2-amino-5-chloro-a-(cyclopropylethynyl)-a-(trifluoromethyl)benzyl alc. (S)-2-Amino-5-chloro-a-(cyclopropylethynyl)-a-(trifluoromethyl)benzyl alc. was prepd. via asym. addn. of (cyclopropyl)ethynylmagnesium chloride or cyclopropylethynyl sodium to 2-amino-5-chloro-2-Ph trifluoromethyl ketone induced by (1R,2S)-N-pyrrolidinylnorephedrine or (+)-N,N-dimethyl-a-(hydroxymethyl)-b-hydroxy-(p-nitrophenyl)ethylamine in the presence of chirality-inducing assistant, such as trifluoroethanol, trichloroethanol, tert-butanol, neoamyl alc., etc. The invention increases the reaction safety by using the base for substitution of lithium butylide or diethylzinc. The invention also has the advantages of low cost of reagents and is suitable for industrial prodn.
¹Ø¼ü´Ê        amino chloro phenyl trifluoromethyl ketone cyclopropylethynyl addn;chiral inducer;chloro amino cyclopropylethynyl trifluoromethyl benzyl alc asym prepn;chiral inducer asym addn medium;
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