发明名称 |
PREPARATION OF ESCITALOPRAM |
摘要 |
A substantially pure (S)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile intermediate for preparing escitalopram is prepared by: a) combining racemic (±)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile with (−)-di-p-toluoyltartaric acid, in a solvent; b) separating a solid phase comprising a salt of (−)-di-p-toluyltartaric acid with (R)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile enantiomer, and a liquid phase comprising a salt of (−)-di-p-toluoyltartaric acid with (S)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxy-butyl]-3-(hydroxymethyl)benzonitrile enantiomer; c) reacting the liquid phase with a base and isolating enantiomerically enriched (S)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile enantiomer; d) combining enantiomerically enriched (S)-enantiomer obtained in c) with (+)-di-p-toluoyltartaric acid, in a solvent; and e) reacting a precipitate from d) with a base.
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申请公布号 |
US2010249438(A1) |
申请公布日期 |
2010.09.30 |
申请号 |
US20100749569 |
申请日期 |
2010.03.30 |
申请人 |
BOLUGODDU VIJAYA BHASKAR;ELATI CHANDRASEKHAR RAVI RAM;CHEEMALAPATI SASI KALA VENKATA ANNAPURNA;PENUMANDLA RAJAGOPAL;CHRISTY ARULNATHAN PRABAKAR;VAKAMUDI LAKSHMI VARA PRASAD SREE NAGA VENKATA |
发明人 |
BOLUGODDU VIJAYA BHASKAR;ELATI CHANDRASEKHAR RAVI RAM;CHEEMALAPATI SASI KALA VENKATA ANNAPURNA;PENUMANDLA RAJAGOPAL;CHRISTY ARULNATHAN PRABAKAR;VAKAMUDI LAKSHMI VARA PRASAD SREE NAGA VENKATA |
分类号 |
C07D307/79 |
主分类号 |
C07D307/79 |
代理机构 |
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代理人 |
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主权项 |
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