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1. 发明申请

US20090270624A1 PROCESS FOR PURIFYING NOROXYMORPHONE COMPOUNDS 有权
标题翻译：净化NOROXYMORPHONE化合物的方法
公开(公告)号：US20090270624A1
公开(公告)日：2009-10-29
申请号：US11815784
申请日：2006-02-09
申请人： Ulrich Weigl , Ulf Kötz , Ilia Freifeld
发明人： Ulrich Weigl , Ulf Kötz , Ilia Freifeld
IPC分类号： C07D221/28
CPC分类号： C07D489/08
摘要： A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, α,β-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a selected noroxymorphone compound in a reaction which converts the hydroxyl groups present in the mixture to leaving groups of the formula —OR2 in which R2 is the introduced radical of the leaving group, (b) these leaving groups are optionally detached again, then (c) the resulting mixture is subjected to a selective hydrogenation, so that a saturated bond is formed in the α,β-position of the unsaturated noroxymorphone compounds and any remaining leaving groups are each converted to a hydroxyl group and then optionally (d) the pure noroxymorphone compound is isolated; processing of the noroxymorphone purified in this way to naltrexone or naloxone or a salt of these compounds or a quaternary derivative of these compounds; pharmaceutical formulations comprising such a compound.
摘要翻译：一种用于纯化植物提取物的方法，该植物提取物主要由去甲羟吗啡酮化合物组成，并且通过（a）在合成选择的去甲吗啉酮化合物中转化植物提取物或后续阶段的产物，作为杂质包含α，β-不饱和的吗啡吗啉化合物在将混合物中存在的羟基转化成离去基团的基团 - 其中R 2是离去基团的引入基团的反应中，（b）这些离去基团再次任选地分离，然后（c）所得混合物进行选择性氢化，使得在不饱和去甲吗啉酮化合物的α，β-位上形成饱和键，并且任何剩余的离去基团各自转化为羟基，然后任选地（d）纯的去甲吗啉酮化合物被分离 ; 以这种方式纯化的诺羟吗啡酮的加工是纳曲酮或纳洛酮或这些化合物的盐或这些化合物的季衍生物; 包含这种化合物的药物制剂。

2. 发明授权

US08227609B2 Process for purifying noroxymorphone compounds 有权
标题翻译：净化去甲吗啉酮化合物的方法
公开(公告)号：US08227609B2
公开(公告)日：2012-07-24
申请号：US11815784
申请日：2006-02-09
申请人： Ulrich Weigl , Ulf Kötz , Ilia Freifeld
发明人： Ulrich Weigl , Ulf Kötz , Ilia Freifeld
IPC分类号： C07D221/22
CPC分类号： C07D489/08
摘要： A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, α,β-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a selected noroxymorphone compound in a reaction which converts the hydroxyl groups present in the mixture to leaving groups of the formula —OR2 in which R2 is the introduced radical of the leaving group, (b) these leaving groups are optionally detached again, then (c) the resulting mixture is subjected to a selective hydrogenation, so that a saturated bond is formed in the α,β-position of the unsaturated noroxymorphone compounds and any remaining leaving groups are each converted to a hydroxyl group and then optionally (d) the pure noroxymorphone compound is isolated; processing of the noroxymorphone purified in this way to naltrexone or naloxone or a salt of these compounds or a quaternary derivative of these compounds; pharmaceutical formulations comprising such a compound.
摘要翻译：一种纯化植物提取物的方法，该方法基本上由去甲羟吗啡酮化合物组成，并且通过（a）在选择的去甲吗啡酮合成中转化植物提取物或后续阶段的产物，作为杂质包含α，β-不饱和的去甲吗啉酮化合物在将该混合物中存在的羟基转化为离去基团，其中R 2是离去基团的引入基团的反应基团的反应中，化合物，（b）这些离去基团再次任选地分离，然后（c）使混合物进行选择性氢化，使得在不饱和去甲羟甲基苯氧基化合物的α，bgr-位上形成饱和键，并且任何剩余的离去基团各自转化为羟基，然后任选地（d）纯的去甲吗啉酮化合物孤立以这种方式纯化的诺羟吗啡酮的加工是纳曲酮或纳洛酮或这些化合物的盐或这些化合物的季衍生物; 包含这种化合物的药物制剂。

3. 发明申请

US20130005001A1 METHOD FOR PRODUCING NEBIVOLOL 审中-公开
标题翻译：生产NEBIVOLOL的方法
公开(公告)号：US20130005001A1
公开(公告)日：2013-01-03
申请号：US13574348
申请日：2011-01-21
申请人： Gerhard Jas , Ilia Freifeld , Kurt Kesseler
发明人： Gerhard Jas , Ilia Freifeld , Kurt Kesseler
IPC分类号： C07D407/12 , C12P17/16
CPC分类号： C07D311/58 , C12P17/06 , Y02P20/55
摘要： The present invention relates to a method for producing racemic nebivolol represented by general formula (I) from the enantiomerically-pure compounds represented by formula (IVa) and (IVb); whereby racemic nebivolol is obtained through mixing enantiomerically-pure d-nebivolol and l-nebivolol which are synthesised independent of each other as enantiomerically-pure compounds through individual coupling of the 4 enantiomerically-pure key intermediates represented by formula (IIa-d) to the corresponding precursors represented by formula (IIIa-d); whereby d-nebivolol (Ia) is obtained through coupling (IIa) to (IIIb) or (IIb) to (IIIa) and l-nebivolol (Ib) is obtained through coupling (IIc) to (IIId) or (IId) to (IIIc), and PG in the intermediates represented by formula (IIa-d) is a hydrogen atom or an amine protection group, and X in the precursors represented by formula (IIIa-d) is a halogen atom, a hydroxyl group, an acyl group, an alkylsulfonyloxy group or an arylsulfonyloxy group, whereby intermediate (IIa) is formed from (IIIa), intermediate (IIb) is formed from (IIIb), intermediate (IIc) is formed from (IIIc), and intermediate (IId) is formed from (IIId), whereby the precursors represented by formula (IIIa) and (IIId) originate from the ketone precursor represented by formula (IVa), and the precursors represented by formula (IIIb) and (IIIc) originate from the ketone precursor represented by formula (IVb), and Z in the ketone precursors (IVa,b) is a halogen atom, a hydroxyl function, an acyl group, an alkylsulfonyloxy group or an arylsulfonyloxy group.
摘要翻译：本发明涉及由式（IVa）和（IVb）表示的对映体纯的化合物制备由通式（I）表示的外消旋的奈比洛尔的方法; 由此通过混合对映异构纯的d-内比洛尔和1-内啡洛，通过将由式（IIa-d）表示的4种对映异构纯的关键中间体与式（IIa-d）表示的单独偶联作为对映异构体纯的化合物彼此独立地合成而获得外消旋奈必洛尔由式（IIIa-d）表示的相应前体; 其中通过偶联（IIa）至（IIIb）或（IIb）至（IIIa）获得了d-奈必洛尔（Ia），通过偶联（IIc）至（IIId）或（IId）至 IIIa）和由式（IIa-d）表示的中间体中的PG是氢原子或胺保护基，并且由式（IIIa-d）表示的前体中的X是卤素原子，羟基，酰基基团，烷基磺酰氧基或芳基磺酰氧基，由（IIIa）形成中间体（IIa），中间体（IIb）由（IIIb）形成，中间体（IIc）由（IIIc）形成，中间体（IId）由（IIId）形成，其中由式（IIIa）和（IIId）表示的前体源自由式（IVa）表示的酮前体，由式（IIIb）和（IIIc）表示的前体源自代表的通过式（IVb），酮前体（IVa，b）中的Z为卤素原子，羟基官能团，酰基，烷基磺酰氧基团 p或芳基磺酰氧基。

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