利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

2 条记录 (耗时 0.008 秒)

    A METHOD FOR THE PREPARATION OF (S)-N-METHYL-3-(l-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE)
    1.
    发明公开
    A METHOD FOR THE PREPARATION OF (S)-N-METHYL-3-(l-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE) 有权
    工艺用于制备（S）-N-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺盐酸盐（度洛西汀）

    公开(公告)号：EP1968965A2

    公开(公告)日：2008-09-17

    申请号：EP06840860.8

    申请日：2006-12-22

    申请人： Zentiva, a.s.

    发明人： RIDVAN, Ludek ,  JARRAH, Kamal ,  CINIBULK, Josef ,  ZATOPKOVA, Monika ,  PLACEK, Lukas

    IPC分类号： C07D333/20

    CPC分类号： C07D333/20

    摘要： A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-mienyl)propylamine of Formula(l) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)-N, N-dimethyl-3-(l-naρhthyloxy)-3-(2-th1enyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(l-naphthyloxy)- 3-(2-thienyl)propylamine and D- tartaric acid (2:1), b) isolation of the salt (S)-N, N-dimethyl-3-(naphthyloxy)-3-(2- thienyl)propylamine/D- tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)-N, N-dimethyl-3-(l- naphthyloxy)-3-(2-thienyl) propylamine by action of an inorganic or organic base, c) demethylation of (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2- thienyl) propylamine by action of an alkylchloroformate of formula C1COOR (R=C1-C5 alkyl, or C6-C12 aryl or alkylraryl), especially phenyl, ethyl or methyl chloroformate, and d) hydrolytic release of the duloxetine base of formula I and optionally conversion of the base to a salt with the respective acid, or salt of a weak base.

    METHODE OF MANUFACTURING GLIMEPIRIDE AND THE RESPECTIVE INTERMEDIATE
    2.
    发明公开
    METHODE OF MANUFACTURING GLIMEPIRIDE AND THE RESPECTIVE INTERMEDIATE 审中-公开
    用于生产格列美脲和相关中间体

    公开(公告)号：EP1594839A2

    公开(公告)日：2005-11-16

    申请号：EP04712991.1

    申请日：2004-02-20

    申请人： Zentiva, a.s.

    发明人： RADL, Stanislav ,  JARRAH, Kamal

    IPC分类号： C07D207/38 ,  C07C211/35

    CPC分类号： C07C211/35 ,  C07B2200/07 ,  C07D207/38

    摘要： A method of manufacturing glimepiride of formula I wherein trans-4-methylcyclohexylamine pivalate of formula (VII) is reacted, either directly or after conversion to trans-4-methylcyclohexylamine or to its another salt, with an alkyl [4-(2-{[(3-ethyl-4-methyl-2-oxo-2,5-dihydro-lH-pyrrol-l yl)carbonyl]amino)ethyl)phenyl]-sulfonyl carbamate of general formula (IV) wherein R is a C1-C5 alkyl, giving glimepiride of formula I. trans-4-Methylcyclohexylamine pivalate of formula (VII).