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1. 发明申请

US20050228198A1 Manufacture of phenyl ethylamine compounds, in particular venlafaxine 失效
标题翻译：制造苯乙胺化合物，特别是文拉法辛
公开(公告)号：US20050228198A1
公开(公告)日：2005-10-13
申请号：US10508930
申请日：2002-06-13
申请人： Jagdish Saigal , Rajender Gupta , Vilas Pandit , Anand Desai , Navneet Mehta , Shrikant Rane
发明人： Jagdish Saigal , Rajender Gupta , Vilas Pandit , Anand Desai , Navneet Mehta , Shrikant Rane
IPC分类号： C07C29/48 , C07C209/48 , C07C213/02 , C07C213/08 , C07C215/42 , C07C217/60 , C07C217/74
CPC分类号： C07C209/48 , C07C213/02 , C07C213/08 , C07C2601/14 , C07C215/42 , C07C217/60 , C07C217/74
摘要： A process for the preparation of hydroxy(cycloalkane/cyclokene)phenylethyl of the general formula (III) comprising alkylation of its precursor amine of general formula (II) which is in turn produced by an effective reduction process from its precursor cyanide having the general formula (I) using Raney Nickel (CORMIII) as catalyst where, either of R5 and R6 independently could be in meta or para position and R5, R6 are independently hydrogen, hydroxyl, alkyl, alkanoyloxy, cyano nitro, alkylmercapto, amino, alkylamino, alkanamido, halo, trifluoromethyl, or taken together methylenedioxy, n is 0, 1, 2, 3, 4; R7 is hydrogen of alkyl of 1-7 carbon atom, R1 IH or alkyl of 1-3 carbon atom and R2 is alkyl 1-3 carbon atom, the dotted line represents optional unsaturation. Compounds of formulae IV, V and VI are respectively derivatives of compounds I, II and III respectively.
摘要翻译：制备通式（III）的羟基（环烷烃/环烯）苯乙基的方法，包括其通式（II）的前体胺的烷基化反应，其通过有效的还原方法从其具有通式（II）的前体氰化物（I）使用阮内镍（CORIII）作为催化剂，其中R 5和R 6中的任一个可以独立地为间位或对位，R 5，R 6独立地为氢，羟基，烷基，烷酰氧基，氰基硝基，烷基巯基，氨基，烷基氨基，烷酰氨基，卤素，三氟甲基或亚甲二氧基取代，n为0,1,2,3,4; R7是1-7个碳原子的烷基，R1H或1-3个碳原子的烷基，R2是烷基1-3个碳原子的氢，虚线代表任选的不饱和键。式IV，V和VI的化合物分别是化合物I，II和III的衍生物。

2. 发明申请

US20050119503A1 Process for preparation of gabapentin 失效
标题翻译：加巴喷丁的制备方法
公开(公告)号：US20050119503A1
公开(公告)日：2005-06-02
申请号：US10497899
申请日：2002-11-18
申请人： Jagdish Saigal , Rajender Gupta , Rajesh Naik , Araddy Rajshekhar , Rajesh Joshi
发明人： Jagdish Saigal , Rajender Gupta , Rajesh Naik , Araddy Rajshekhar , Rajesh Joshi
IPC分类号： A61K31/195 , C07C227/38 , C07C227/42
CPC分类号： C07C227/42 , C07C229/28
摘要： A process for producing Gabapentin, (1-(anminomethyl)-1-cyclohexaneacetic acid) from Gabapentin hydrochloride salt. In the process the Gabapentin hydrochloride is converted to Gabapentin using inorganic base such as Barium hydroxide. Gabapentin hydrochloride is converted to Gabapentin sulfate which in turn is converted to free base using Barium hydroxide. The process is directed to improvement in the manufacture of Gabapentin which would be industrially feasible and effective Gabapentin obtained following the process of the invention is suitable as a drug especially in the treatment of cerebral diseases such as epilepsy. The above process involves simple steps and avoid the problems of the known art. In particular the process avoids severe conditions and/or complexities and can be readily adopted for industrial application. The process provides for good yield and does not involve lengthy extended process steps. It is cost-effective and can be carried out involving simple ingredients and steps of manufacture.
摘要翻译：从加巴喷丁盐酸盐制备加巴喷丁（1-（氨基甲基）-1-环己烷乙酸）的方法。在该过程中，使用无机碱如氢氧化钡将盐酸加巴喷丁转化为加巴喷丁。将加巴喷丁盐酸盐转化为硫酸氢巴比坦，然后使用氢氧化钡将其转化为游离碱。本发明涉及在工业上可行且有效的加巴喷丁的制造方面的改进。本发明方法获得的加巴喷丁适合作为特别是治疗脑疾病如癫痫的药物。上述过程涉及简单的步骤并且避免了已知技术的问题。特别地，该方法避免了苛刻的条件和/或复杂性，并且可以容易地用于工业应用。该方法提供良好的产率，并不涉及冗长的扩展工艺步骤。它具有成本效益，可以进行简单的成分和制造步骤。

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