发明名称 METHOD OF PRODUCING ACETATE SALT OF METHYL ESTER OF (2R,3S)-3-PHENYLISOSERINE
摘要 FIELD: chemistry. ^ SUBSTANCE: invention relates to a method for anantioselective production of an acetate salt of methyl ester of (2R,3S)-3-phenylisoserine of formula (I), which is a structural element suitable for use in synthesis of taxane derivatives. The method involves the following steps: a) treating racemic treo-3-phenylisoserine amide (VI) with an enantiomerically pure acid to obtain the corresponding salt formed from (2R,3S)-3-phenylisoserine amide and acid; b) treating the salt formed from (2R,3S)-3-phenylisoserine amide and acid with a strong inorganic acid in a protonic solvent to obtain a salt formed from (2R,3S)-3-phenylisoserine amide and inorganic acid; c) treating the salt formed from (2R,3S)-3-phenylisoserine amide and inorganic acid with hydrochloric acid in a protonic solvent with subsequent treatment with acetic acid to crystallise an acetate salt of methyl ester of (2R,3S)-3-phenylisoserine amide. The invention also relates to an intermediate compound, specifically (2R,3S)-3-phenylisoserine amide in form of a salt of (-) dibenzoyl tartaric acid. ^ EFFECT: method for enantioselective production of an acetate salt of methyl ester of (2R,3S)-3-phenylisoserine amide of formula (I). ^ 4 cl, 6 ex
申请公布号 RU2459802(C2) 申请公布日期 2012.08.27
申请号 RU20090131595 申请日期 2008.02.11
申请人 INDENA S.P.A. 发明人 CHICHERI DANIELE;GABETTA BRUNO;VIN'OLA NIKOLA;MITTSEL' FRIDER;VEBER BEAT T.
分类号 C07C227/18 主分类号 C07C227/18
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