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1. 发明申请

US20110077405A1 PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE (S)-1-PHENYI-1,2,3,4- TETRAHYDROISOQUINOLINE 审中-公开
标题翻译：制备纯度（S）-1-苯基-1,2,3,4-四氢喹啉的方法
公开(公告)号：US20110077405A1
公开(公告)日：2011-03-31
申请号：US12993874
申请日：2009-05-22
申请人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
发明人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
IPC分类号： C07D453/02 , C07D217/02
CPC分类号： C07D217/02
摘要： Process for preparation of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline wherein 1-phenyl-1,2,3,4-tetrahydroisoquinoline is reacted with D-(−)-tartaric acid in a solvent system comprising of methanol and water, preferably at 3.3:1 to 1:1 volume ratio, the crystallization mixture is left for crystallization and (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline is released from obtained crystalline diastereoisomeric salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline is the intermediate in enantiomeric synthesis of solifenacin.
摘要翻译：（S）-1-苯基-1,2,3,4-四氢异喹啉的制备方法，其中1-苯基-1,2,3,4-四氢异喹啉与D - （ - ） - 酒石酸在溶剂体系中反应包括甲醇和水，优选以3.3:1至1:1的体积比，结晶混合物留下结晶，（S）-1-苯基-1,2,3,4-四氢异喹啉从得到的结晶非对映异构体盐按照标准程序。（S）-1-苯基-1,2,3,4-四氢异喹啉是solifenacin对映体合成中的中间体。

2. 发明申请

US20090105483A1 PROCESS FOR THE PREPARATION OF PRAMIPEXOLE BASE AND/OR ITS SALTS 审中-公开
标题翻译：制备原料和/或其盐的方法
公开(公告)号：US20090105483A1
公开(公告)日：2009-04-23
申请号：US12164005
申请日：2008-06-28
申请人： Roman BALICKI , Michal ODROWAZ-SYPNIEWSKI , Agnieszka CIESIELSKA , Wieslaw SZELEJEWSKI , Joanna ZAGRODZKA , Grazyna CIEPLUCHA
发明人： Roman BALICKI , Michal ODROWAZ-SYPNIEWSKI , Agnieszka CIESIELSKA , Wieslaw SZELEJEWSKI , Joanna ZAGRODZKA , Grazyna CIEPLUCHA
IPC分类号： C07D277/82
CPC分类号： C07D277/82
摘要： The process for the preparation of pramipexole base and/or its pharmaceutically acceptable salts, especially the hydrochloride salt, in the alkylation reaction of (S)-(−)2,6-diamino-4,5,6,7-tetrahydrobenzothiazole with an alkylating agent, wherein the reaction is carried out in the absence of a base, and in a solvent from which the resulting N-monoalkylated product selectively precipitates out as a salt. After isolation from the reaction mixture, the N-monoalkylated product is converted a) into the free pramipexole base upon treatment with an inorganic base and is then converted into another pharmaceutically acceptable pramipexole salt; or b) directly into another pharmaceutically acceptable pramipexole salt or the hydrate thereof.
摘要翻译：在（S） - （ - ） - 2,6-二氨基-4,5,6,7-四氢苯并噻唑的烷基化反应中制备普拉克索碱和/或其药学上可接受的盐，特别是盐酸盐的方法，烷基化剂，其中反应在不存在碱的情况下进行，在所得的N-单烷基化产物作为盐选择性地析出的溶剂中进行。从反应混合物中分离出来之后，将N-单烷基化产物在无机碱处理后转化为游离的普拉克索碱，然后转化为另一种药学上可接受的普拉克索盐; 或b）直接转化成另一种药学上可接受的普拉克索盐或其水合物。

3. 发明授权

US08436182B2 Process for preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity 有权
标题翻译：制备高度药物纯度的索非那新和/或其药学上可接受的盐的方法
公开(公告)号：US08436182B2
公开(公告)日：2013-05-07
申请号：US12993988
申请日：2009-05-22
申请人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
发明人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
IPC分类号： C07D217/02
CPC分类号： C07D453/02
摘要： A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presence of strong base in polar organic solvent is subject to acylation with (S)-1-phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98%, while maintaining constant anion excess in a reaction mixture, and after reaction completion solifenacin base is optionally transformed into solifenacin salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98% is obtained in a reaction of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline and molar excess of phosgene in a presence of tertiary aromatic amine in aromatic hydrocarbon, and isolated in a crystalline form.
摘要翻译：制备索非那嗪和/或其药学上可接受的高度药学上可接受的盐的方法的特征在于3-（R） - 奎宁环氧基阴离子在极性强碱存在下由3-（R） - 奎宁环醇原位产生有机溶剂用化学纯度至少为98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯进行酰化，同时在反应混合物中保持恒定的阴离子过量，反应完成后，solifenacin碱为任选地根据标准程序转化为索非那新盐。在（S）-1-苯基-1,2,3,4-四氢异喹啉和摩尔（R）的反应中获得化学纯度至少98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯在芳族烃中存在叔芳族胺的过量的光气，并以结晶形式分离。

4. 发明申请

US20110065922A1 Process for Preparation Of Solifenacin and/or the Pharmaceutically Acceptable Salts Thereof of High Pharmaceutical Purity 有权
标题翻译： Solifenacin和/或其高药物纯度的药学上可接受的盐的制备方法
公开(公告)号：US20110065922A1
公开(公告)日：2011-03-17
申请号：US12993988
申请日：2009-05-22
申请人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
发明人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presence of strong base in polar organic solvent is subject to acylation with (S)-1-phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98%, while maintaining constant anion excess in a reaction mixture, and after reaction completion solifenacin base is optionally transformed into solifenacin salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98% is obtained in a reaction of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline and molar excess of phosgene in a presence of tertiary aromatic amine in aromatic hydrocarbon, and isolated in a crystalline form.
摘要翻译：制备索非那嗪和/或其药学上可接受的高度药学上可接受的盐的方法的特征在于3-（R） - 奎宁环氧基阴离子在极性强碱存在下由3-（R） - 奎宁环醇原位产生有机溶剂用化学纯度至少为98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯进行酰化，同时在反应混合物中保持恒定的阴离子过量，反应完成后，solifenacin碱为任选地根据标准程序转化为索非那新盐。在（S）-1-苯基-1,2,3,4-四氢异喹啉和摩尔（R）的反应中获得化学纯度至少98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯在芳族烃中存在叔芳族胺的过量的光气，并以结晶形式分离。

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