-
公开(公告)号：US20180244714A1
公开(公告)日：2018-08-30
申请号：US15553301
申请日：2016-02-26
申请人： Katarzyna KOZIAK , Krzysztof BOJAKOWSKI , Magdalena KOWALEWSKA , Dorota MACIEJKO , Oliwia ZEGROCKA-STENDEL , Iwona GRABOWSKA , Grzegorz GRYNKIEWICZ , Mariusz Marek GRUZA , Kamil JATCZAK , Katarzyna FILIP , Piotr CMOCH , Marta LASZCZ , Instytut Farmaceutyczny
发明人： Katarzyna Koziak , Krzysztof Bojakowski , Magdalena Kowalewska , Dorota Maciejko , Oliwia Zegrocka-Stendel , Iwona Grabowska , Grzegorz Grynkiewicz , Mariusz Marek Gruza , Kamil Jatczak , Katarzyna Filip , Piotr Cmoch , Marta Laszcz
CPC分类号： C07J63/008 , A61K31/58
摘要： Described herein is compound including a protoescigenin derivative having pharmacological properties. Also described are a process of its preparation, and the use of such a compound as a medicament, especially for treating vascular disorders. A pharmaceutical composition comprising such compound is further described.
-
2.发明申请PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE (S)-1-PHENYI-1,2,3,4- TETRAHYDROISOQUINOLINE 审中-公开制备纯度（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
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。
-
3.发明授权Process for preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity 有权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
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Process for Preparation Of Solifenacin and/or the Pharmaceutically Acceptable Salts Thereof of High Pharmaceutical Purity 有权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
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。
-
公开(公告)号：US09073813B2
公开(公告)日：2015-07-07
申请号：US13733855
申请日：2013-01-03
发明人： Mariusz Gruza , Oliwia Zegrocka-Stendel , Tomasz Giller , Grzegorz Grynkiewicz , Marta Laszcz , Kamil Jatczak
CPC分类号： C07C29/095 , C07C29/74 , C07C29/78 , C07C31/278 , C07C35/44 , C07J63/00 , C07J63/008
摘要： A process for the preparation of protoescigenin by hydrolysis of escin isolated from Aesculus hippocastanum. The process includes the following steps: a two-step hydrolysis first under acidic and then basic conditions, enrichment of the crude mixture of sapogenins with protoescigenin, an isolation of the mixture of sapogenins in a solid form, and a purification of the obtained solid and isolation of high purity protoescigenin. The invention also relates to protoescigenin monohydrate in a crystalline form and the preparation thereof. Protoescigenin is a polyhydroxy aglycone, which can be used as a synthon in the chemical modifications of naturally occurring saponins.
摘要翻译： 一种通过水解从七叶树七叶皂苷中分离的七叶皂苷制备原丝酵母素的方法。 该方法包括以下步骤：首先在酸性和碱性条件下进行两步水解，将粗皂苷元粗制混合物与原丝酵母素进行富集，分离固体形式的皂角蛋白的混合物，以及所得固体和 隔离高纯度原丝酵母。 本发明还涉及结晶形式的原生精皮质素一水合物及其制备。 原花青素是多羟基苷元，可用作天然皂苷的化学修饰中的合成子。
-
-
-
-
搜索结果
5 条记录 (耗时 0.03 秒)
