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1. 发明授权

US06555665B1 Glycosidation of 4,5-epoxymorphinan-6-ols 失效
标题翻译： 4,5-环氧吗啡喃-6-ols的糖化
公开(公告)号：US06555665B1
公开(公告)日：2003-04-29
申请号：US09601358
申请日：2000-09-15
申请人： Arie Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rochman
发明人： Arie Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rochman
IPC分类号： C07H1500
CPC分类号： C07H17/00
摘要： Glycosidation of 4,5-Epoxymorphinan-6-ols with a Thioglycoside as a glycoside donor is disclosed. The process comprises reacting a 4,5-Epoxymorphinan-6-ol and a Thioglycoside in the presence of a thiophilic promoter under conditions capable of forming 4,5-Epoxymorphinan-6-glycosides. This novel approach was used for preparation of pharmaceutically important 4,5-Epoxymorphinan-6-&bgr;-D-glucuronides. The process provides both high stereo-selectivity and high yields.
摘要翻译：公开了以硫代糖苷作为糖苷供体的4,5-环氧基吗啡喃-6-ols的糖苷化。该方法包括在能够形成4,5-环氧吗啡喃-6糖苷的条件下，在一种嗜碱性启动子存在下使4,5-环氧吗啡喃-6-醇与硫代糖苷反应。该新方法用于制备药物重要的4,5-环氧吗啡喃-6-β-D-葡糖苷酸。该方法提供高立体选择性和高产率。

2. 发明授权

US06737518B1 Process for preparation of 4,5-epoxymorphinan-6-oxyglucuronides 失效
标题翻译：制备4,5-环氧吗啡喃-6-氧基葡糖苷酸的方法
公开(公告)号：US06737518B1
公开(公告)日：2004-05-18
申请号：US09700035
申请日：2001-05-18
申请人： Arie L. Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rokhman
发明人： Arie L. Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rokhman
IPC分类号： C07H1500
CPC分类号： C07H17/08
摘要： Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5-Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.
摘要翻译：公开了在能够形成4,5-环氧基吗啡喃-6-氧基葡糖苷酸的条件下，在含锌化合物作为活化剂的情况下，将4,5-环氧吗啡喃-6-ols与溴葡萄糖苷酸缀合。这种新方法提供了一种制备4,5-环氧吗啡喃-6-氧基葡糖苷酸的两种端基异构体的有效方法。去保护的最终产物可用作止痛剂。

3. 发明申请

US20050049302A1 Process for the preparation of dronedarone 失效
标题翻译：制备决奈达隆的方法
公开(公告)号：US20050049302A1
公开(公告)日：2005-03-03
申请号：US10494960
申请日：2002-11-06
申请人： Arie Gutman , Gennadi Nisnevich , Lev Yudovitch
发明人： Arie Gutman , Gennadi Nisnevich , Lev Yudovitch
IPC分类号： C07D307/79 , C07D307/80 , C07D307/87 , A61K31/343
CPC分类号： C07D307/79 , C07D307/80
摘要： The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.
摘要翻译：根据本发明的一个方面，本发明提供了制备决奈达隆[1]及其药学上可接受的盐的新方法。根据优选的实施方案，该方法包括对乙氧基苯胺或对苯乙胺与乙酸酐的N-乙酰化反应，所得的N-（4-烷氧基苯基）乙酰胺与氯化2-氯己酰氯在溴化铝存在下反应得到N- [3-（2-溴己酰基）-4-羟基苯基]乙酰胺[6a]，将化合物[6a]转化为2-丁基-5-苯并呋喃胺盐酸盐[12a]，随后将[12a]转化为[1 ]或其药学上可接受的盐。根据本发明的另一方面，提供了新的中间体，特别是新化合物[6a]和[12a]。本发明的新型中间体是稳定的固体化合物，其可以高产率获得，其可以通过结晶容易地纯化并长时间储存。

4. 发明授权

US07157590B2 Process for the preparation of 17-phenyl-18,19,20-thinor-pgf 2a and its derivatives 有权
标题翻译：制备17-苯基-18,19,20-薄-orf-2a及其衍生物的方法
公开(公告)号：US07157590B2
公开(公告)日：2007-01-02
申请号：US10478849
申请日：2002-05-03
申请人： Arie Gutman , Gennady Nisnevich , Marina Etinger , Igor Zaltzman , Lev Yudovitch , Boris Pertsikov
发明人： Arie Gutman , Gennady Nisnevich , Marina Etinger , Igor Zaltzman , Lev Yudovitch , Boris Pertsikov
IPC分类号： C07C51/36
CPC分类号： C07C405/00
摘要： The present invention provides a new and effective process for the synthesis of 17-phenyl-18,19,20-trinor-PGF2α and its derivatives, including the anti-glaucoma drugs Bimatoprost and Latanoprost. The benefit of the present invention rises inter alia from the fact that a major intermediate involved in the synthesis of the above compounds may be isolated from a mixture containing also an undesired isomer, by crystallization. In addition, the undesired isomer may be oxidized to give the starting compound, which is then recycled.
摘要翻译：本发明提供了一种新的和有效的合成17-苯基-18,19,20-三磷酸-PGF2α及其衍生物的方法，包括抗青光眼药物比马前列素和拉坦前列素。本发明的优点尤其在于通过结晶从参与合成上述化合物的主要中间体也可以从含有不想要的异构体的混合物中分离出来。此外，不需要的异构体可被氧化，得到起始化合物，然后再循环。

5. 发明授权

US07312345B2 Process for the preparation of dronedarone 失效
标题翻译：制备决奈达隆的方法
公开(公告)号：US07312345B2
公开(公告)日：2007-12-25
申请号：US10494960
申请日：2002-11-06
申请人： Arie Gutman , Gennadi Nisnevich , Lev Yudovitch
发明人： Arie Gutman , Gennadi Nisnevich , Lev Yudovitch
IPC分类号： C07D307/81 , C07D307/83 , C07C233/25 , C07C271/28 , C07C271/58
CPC分类号： C07D307/79 , C07D307/80
摘要： The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.
摘要翻译：根据本发明的一个方面，本发明提供了制备决奈达隆[1]及其药学上可接受的盐的新方法。根据优选的实施方案，该方法包括对乙氧基苯胺或对苯乙胺与乙酸酐的N-乙酰化反应，所得的N-（4-烷氧基苯基）乙酰胺与氯化2-氯己酰氯在溴化铝存在下反应得到N- [3-（2-溴己酰基）-4-羟基苯基]乙酰胺[6a]，将化合物[6a]转化为2-丁基-5-苯并呋喃胺盐酸盐[12a]，随后将[12a]转化为[1 ]或其药学上可接受的盐。根据本发明的另一方面，提供了新的中间体，特别是新化合物[6a]和[12a]。本发明的新型中间体是稳定的固体化合物，其可以高产率获得，其可以通过结晶容易地纯化并长时间储存。

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