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1. 发明申请

WO2002046153A3 PROCESS FOR THE PREPARATION OF ZAFIRLUKAST 审中-公开
公开(公告)号：WO2002046153A3
公开(公告)日：2002-06-13
申请号：PCT/IB2001/002268
申请日：2001-11-30
申请人： ISP FINETECH LTD. , GUTMAN, Arie , NISNEVICH, Gennady , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim
发明人： GUTMAN, Arie , NISNEVICH, Gennady , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim
IPC分类号： C07D209/18
摘要： The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole,(b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a), (d) isolating the salt of (indol-3-ylmethyl)benzoic acid and/or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or its salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [1a] is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.

2. 发明申请

WO0246153A2 PROCESS FOR THE PREPARATION OF ZAFIRLUKAST 审中-公开
标题翻译：制备ZAFIRLUKAST的方法
公开(公告)号：WO0246153A2
公开(公告)日：2002-06-13
申请号：PCT/IB0102268
申请日：2001-11-30
申请人： ISP FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
发明人： GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
IPC分类号： C07D209/18 , C07D209/24 , C07D209/00
CPC分类号： C07D209/18 , C07D209/24 , Y02P20/582
摘要： The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole,(b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a),(d) isolating the salt of (indol-3-ylmethyl)benzoic acid and/or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or it's salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [1a] is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.
摘要翻译：本发明提供了一种制备烷基（1-烷基吲哚-3-基甲基）苯甲酸酯衍生物的新方法，该方法包括以下步骤：（a）使（卤代甲基）烷基烷基酯与过量的吲哚反应，所述吲哚为在吲哚的3位上促进烷基化的条件下，在位置1-，2-和3-未被取代，得到包含烷基（吲哚-3-基甲基）苯甲酸酯和未反应的起始吲哚的混合物，（b）处理得到的混合物在步骤（a）中与碱反应以产生包含（吲哚-3-基甲基）苯甲酸的盐和未反应的吲哚的混合物，（c）从步骤（b）中获得的混合物中回收未反应的吲哚，并将吲哚作为步骤（a）的起始原料，（d）分离（吲哚-3-基甲基）苯甲酸的盐和/或酸化盐以形成（吲哚-3-基甲基）苯甲酸，（e）使吲哚-3-基甲基）苯甲酸或其与烷基化剂的盐在碱的存在下形成所需的烷基（1-alkylindol -3-基甲基）苯甲酸甲酯。上述方法还提供了抗哮喘白三烯拮抗剂扎非司酮的制备。在这种情况下，在该方法的步骤（e）中形成3-甲氧基-4-（1-甲基-5-硝基吲哚-3-基甲基）苯甲酸甲酯[1a]，该化合物随后通过已知方法转化成扎非司酮。

3. 发明申请

WO2002068376A1 PROCESS FOR THE PREPARATION OF RASAGILINE AND ITS SALTS 审中-公开
标题翻译：制备RASAGILINE及其盐的方法
公开(公告)号：WO2002068376A1
公开(公告)日：2002-09-06
申请号：PCT/IB2002/000542
申请日：2002-02-25
申请人： ISP FINETECH LTD. , GUTMAN, Arie, L. , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim , NISNEVICH, Gennady
发明人： GUTMAN, Arie, L. , ZALTZMAN, Igor , PONOMAREV, Victor , SOTRIHIN, Maxim , NISNEVICH, Gennady
IPC分类号： C07C211/42
CPC分类号： C07C209/88 , C07B2200/07 , C07C211/42
摘要： The present invention provides a novel process for the preparation of rasagiline or its salts, in particular rasagiline mesylate, which process comprises the steps of : (a) reacting racemic N-benzyl-1-indanamine with (R,R)-tartaric acid in water; (b) cooling the mixture of step (a) to form a salt of (R)-enantiomerically enriched N-benzyl-1-indanamine with (R,R)-tartaric acid in solid form; (c) separating said precipitated solid obtained in step (b); (d) hydrogenating under catalytic conditions the solid product of step (c), optionally, in the presence of acids, bases or salts; (e) basifying the reaction mixture of step (d) with aqueous base and isolating (R)-enantiomerically enriched 1-indanamine from the obtained mixture; and (f) converting the (R)-enantiomerically enriched 1-indanamine of step (e) to rasagiline or its salts.
摘要翻译：本发明提供了一种制备雷沙吉兰或其盐，特别是甲磺酸雷沙吉兰的新方法，该方法包括以下步骤：（a）使外消旋N-苄基-1-茚胺与（R，R） - 酒石酸反应水; （b）冷却步骤（a）的混合物以形成固体形式的（R） - 对映体富集的N-苄基-1-茚满胺与（R，R） - 酒石酸的盐; （c）分离步骤（b）中获得的沉淀固体; （d）在催化条件下氢化步骤（c）的固体产物，任选地在酸，碱或盐的存在下; （e）将步骤（d）的反应混合物与碱水溶液碱化并从所得混合物中分离（R） - 对映体富集的1-二氮茚; 和（f）将（R） - 对映异构体富集的步骤（e）的1-二胺转化为雷沙吉兰或其盐。

4. 发明申请

WO0238545A3 CRYSTALLINE ETHANOLATE SOLVATE FORM OF ZAFIRLUKAST, PROCESS FOR MANUFACTURE AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译： ZAFIRLUKAST的晶体乙酸盐溶液形式，其制备方法和药物组合物
公开(公告)号：WO0238545A3
公开(公告)日：2002-07-25
申请号：PCT/IL0100982
申请日：2001-10-24
申请人： ISP FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PERTSIKOV BORIS , SOTRIHIN MAXIM , PONOMAREV VICTOR
发明人： GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PERTSIKOV BORIS , SOTRIHIN MAXIM , PONOMAREV VICTOR
IPC分类号： A61P11/06 , C07D209/24 , A61K31/404
CPC分类号： C07D209/24
摘要： A novel, crystalline ethanolate solvate form of zafirlukast is disclosed, as well as methods for preparing it. Pharmaceutical compositions containing this novel form of zafirlukast are also disclosed. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example in the treatment of asthma.
摘要翻译：公开了扎鲁司特的新颖结晶乙醇溶剂化物形式及其制备方法。还公开了含有这种新型扎鲁司特的药物组合物。该组合物可用于治疗涉及白三烯的疾病，例如治疗哮喘。

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