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1. 发明授权

US06500955B1 One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate 失效
标题翻译： [2,8-双（三氟甲基）-4-喹啉基] -2-吡啶基甲酮，甲氟喹中间体
公开(公告)号：US06500955B1
公开(公告)日：2002-12-31
申请号：US10058304
申请日：2002-01-30
申请人： Harmander Pal Singh Chawla , Perminder Singh Johar , Alka Mittal , Ram Avtar Meena , Villendra Singh Negi
发明人： Harmander Pal Singh Chawla , Perminder Singh Johar , Alka Mittal , Ram Avtar Meena , Villendra Singh Negi
IPC分类号： C07D40106
CPC分类号： C07D401/06
摘要： The present invention provides a simple single step process for the preparation of [2,8-bis(trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.
摘要翻译：本发明提供了制备[2,8-双（三氟甲基）-4-喹啉基] -2-吡啶基甲酮的简单的单步方法，包括在存在下将卤代喹啉与α-吡啶甲基衍生物缩合的步骤的溶剂，碱和相转移催化剂在-10℃至+ 90℃

2. 发明申请

US20090281323A1 PROCESS FOR THE MANUFACTURE OF MONTELUKAST SODIUM 审中-公开
标题翻译： MONTELUKAST SODIUM制造工艺
公开(公告)号：US20090281323A1
公开(公告)日：2009-11-12
申请号：US12296644
申请日：2006-09-28
申请人： Harmander Pal Singh Chawla , Anil Shankar Chowdhary , Ajay Mangubhai Patel , Manish Popatlal Patel
发明人： Harmander Pal Singh Chawla , Anil Shankar Chowdhary , Ajay Mangubhai Patel , Manish Popatlal Patel
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： Process for the manufacture of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid, sodium salt [montelukast sodium (I)] consisting of: i. Converting methyl 1-(mercaptomethyl)-cyclopropaneacetate to a metal salt (X) using a metal hydroxide, ii. Subjecting the metal salt (X) to monometallation to provide a dimetallide (XI). iii. Converting a diol of formula (II) to a mesylate of formula (III) and reacting (III) in situ with (XI) affordin the metal salt of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid. iv. Reacting the metal salt in-situ with a base and purifying to afford an amine salt (XII). v. Treating (XII) with a sodium base and precipitating out montelukast sodium (I).
摘要翻译：制备1 - [[（1R）-1- [3 - [（1E）-2-（7-氯-2-喹啉基）乙烯基]苯基] -3- [2-（1-羟基 - 1-甲基乙基）苯基]丙基]硫基]甲基]环丙烷乙酸钠盐[孟鲁司特钠（I）]由以下组成：i。使用金属氢氧化物将1-（巯基甲基） - 环丙烷甲酸甲酯转化为金属盐（X），ii。使金属盐（X）进行单金属化以提供二叠氮化物（XI）。 iii。将式（II）的二醇转化为式（III）的甲磺酸酯并与（XI）原位反应，得到1 - [[（1R）-1- [3 - [（1E） -2-（7-氯-2-喹啉基）乙烯基]苯基] -3- [2-（1-羟基-1-甲基乙基）苯基]丙基]硫基]甲基]环丙烷乙酸。 iv。用碱反应金属盐并纯化得到胺盐（Ⅻ）。 v。用钠碱处理（XII）并沉淀孟鲁司特钠（I）。

3. 发明申请

US20100184990A1 Process for the Manufacture of Flecainide 审中-公开
标题翻译：氟卡胺的制备方法
公开(公告)号：US20100184990A1
公开(公告)日：2010-07-22
申请号：US11988126
申请日：2005-09-09
申请人： Harmander Pal Singh Chawla , Anil Shankar Chowdhary , Piyush Bhikhubhai Limbad , Rajesh Jagannathbhai Jha , Vipul Narbheshankar Joshi
发明人： Harmander Pal Singh Chawla , Anil Shankar Chowdhary , Piyush Bhikhubhai Limbad , Rajesh Jagannathbhai Jha , Vipul Narbheshankar Joshi
IPC分类号： C07D213/46
CPC分类号： C07D213/40
摘要： The invention describes an improved process for the manufacture of a Flecainide intermediate viz N-(pyridin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide (II). It consists of reacting 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with an acid chloride in a solvent mixture in presence of a base at −10 to −50° C. The resulting mixed anhydride is then condensed with 2-aminomethylpyridine at −10 to −40° C. and the resulting product after aqueous workup is purified by crystallization. This affords the intermediate II in vastly improved yields and quality. The intermediate II on catalytic hydrogenation affords N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide (Flecainide), isolated as its acetate.
摘要翻译：本发明描述了制备N-（吡啶-2-基甲基）-2,5-双（2,2,2-三氟乙氧基）苯甲酰胺（II）的氟卡尼定中间体的改进方法。它由在-10至-50℃的碱存在下在溶剂混合物中使2,5-双（2,2,2-三氟乙氧基）苯甲酸与酰氯反应。然后将所得混合酸酐与 2-氨基甲基吡啶在-10至-40℃下，并且水处理后的所得产物通过结晶纯化。这为中间体II提供了极大提高的产量和质量。催化氢化的中间体II提供作为其乙酸酯分离的N-（2-哌啶基甲基）-2,5-双（2,2,2-三氟乙氧基）苯甲酰胺（Ficarainide）。

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