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1. 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。

2. 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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