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1. 发明申请

WO2007116240A1 AN IMPROVED PROCESS FOR THE MANUFACTURE OF MONTELUKAST SODIUM 审中-公开
标题翻译：改进的MONTELUKAST SODIUM制造工艺
公开(公告)号：WO2007116240A1
公开(公告)日：2007-10-18
申请号：PCT/IB2006/002690
申请日：2006-09-28
申请人： GLADE ORGANICS PRIVATE LIMITED , CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Ajay, Mangubhai , PATEL, Manish, Popatlal
发明人： CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Ajay, Mangubhai , PATEL, Manish, Popatlal
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）。

2. 发明申请

WO2007072114A1 AN IMPROVED PROCESS FOR THE MANUFACTURE OF MONTELUKAST SODIUM 审中-公开
标题翻译：改进的MONTELUKAST SODIUM制造工艺
公开(公告)号：WO2007072114A1
公开(公告)日：2007-06-28
申请号：PCT/IB2006/000059
申请日：2006-01-16
申请人： GLADE ORGANICS PRIVATE LIMITED , CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Ajay, Mangubhai , JOSHI, Vipul, Narbheshankar , PATEL, Manish, Popatlal
发明人： CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Ajay, Mangubhai , JOSHI, Vipul, Narbheshankar , PATEL, Manish, Popatlal
IPC分类号： C07D215/18 , C07B45/06
CPC分类号： C07D215/18
摘要： An improved 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)]. It consists of converting a vital intermediate 1-(mercaptomethyl)-cyclopropane acetic acid of formula IX, to a quaternary ammonium salt of formula X, using a suitable base in a suitable solvent at 0°C to 50°C followed by monometalation to provide an intermediate of formula XI and subsequent condensation of XI with 2-[2-[3-(S)-[3-[2-(7-chloro-2-quinolinyl)-ethenyl] phenyl]-3-methanesulphonyloxypropyl] phenyl]-2-propanol at 0 to -50°C to afford 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 as the quaternary ammonium salt which is filtered, purified by crystallization from a suitable solvent and finally treated with a sodium base in a suitable solvent to generate montelukast sodium which is isolated by trituration with an antisolvent. The invention provides a convenient process for preparing montelukast sodium (I) in good yields and purities.
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）]。它包括将式IX的重要中间体1-（巯基甲基） - 环丙烷乙酸转化成式X的季铵盐，使用合适的碱在合适的溶剂中在0℃至50℃下进行单金属化，从而提供式XI的中间体，随后XI与2- [2- [3-（S） - [3- [2-（7-氯-2-喹啉基） - 乙烯基]苯基] -3-甲磺酰氧基丙基]苯基] -2-丙醇，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]硫代]甲基]环丙烷乙酸作为季铵盐，将其过滤，通过从合适的溶剂中结晶纯化，最后在合适的溶剂中用钠碱处理产生通过用抗溶剂研磨分离的孟鲁司特钠。本发明提供了以良好的产量和纯度制备孟鲁司特钠（I）的方便的方法。

3. 发明申请

WO2006131782A1 PROCESS FOR THE MANUFACTURE OF METHYL-2-(3-(2-(7-CHLORO-2-QUINOLINYL-ETHENYL)-PHENYL)-3-OXOPROPYL) BENZOATE 审中-公开
标题翻译：甲基-2-（3-（2-（7-氯-2-喹啉基 - 乙烯基） - 苯基）-3-氧代吡咯烷基）苯甲酸酯的制备方法
公开(公告)号：WO2006131782A1
公开(公告)日：2006-12-14
申请号：PCT/IB2005/002705
申请日：2005-09-08
申请人： GLADE ORGANICS PRIVATE LIMITED , PAREKH, Sandip, Jayant , CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Ajay, Mangubhai
发明人： PAREKH, Sandip, Jayant , CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Ajay, Mangubhai
IPC分类号： C07D215/18 , C07B37/02
CPC分类号： C07D215/18
摘要： A process for the preparation of methyl 2-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-oxopropyl)benzoate of the formula II in high yield and purity.
摘要翻译：以高产率和纯度制备式II的2-（3-（2-（3-（2-（7-氯-2-喹啉基） - 乙烯基）苯基）-3-氧代丙基）苯甲酸甲酯的方法。

4. 发明申请

WO2007099388A1 AN IMPROVED PROCESS FOR THE MANUFACTURE OF TOPIRAMATE 审中-公开
标题翻译：用于制备TOPIRAMATE的改进方法
公开(公告)号：WO2007099388A1
公开(公告)日：2007-09-07
申请号：PCT/IB2006/000887
申请日：2006-04-17
申请人： GLADE ORGANICS PRIVATE LIMITED , CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Suhas, Mafatlal , VYAS, Kaushal, Rameshchandra
发明人： CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, Shankar , PATEL, Suhas, Mafatlal , VYAS, Kaushal, Rameshchandra
IPC分类号： C07H9/04 , C07H1/00
CPC分类号： C07H9/04 , C07H1/00
摘要： An improved process for the manufacture of 2,3:4,5-bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate, viz. Topiramate is reported. It consists of subjecting an intermediate of the formula 2,3:4,5-bis-O-(1-methylethylidene)-β-D-fructopyranose to a sulfamoylation reaction with sulfamoyl halide in a suitable solvent of high dielectric constant and in presence of a suitable organic base at a temperature from -50 to 100 C followed by extraction and crystallization to afford a crude product which is finally crystallized from a solvent to afford the title derivative in vastly improved yields and quality. Further the process affords the title compound possessing a good stability.
摘要翻译：制备2,3：4,5-双-O-（1-甲基亚乙基）-β-D-吡喃葡萄糖氨基磺酸酯的改进方法，托吡酯被报道。它包括使式2,3：4,5-双-O-（1-甲基亚乙基）-β-D-吡喃葡萄糖的中间体在高介电常数和存在的适当溶剂中与氨磺酰卤进行氨基甲酰化反应的合适的有机碱在-50至100℃的温度下进行萃取和结晶，得到最终从溶剂中结晶的粗产物，得到极大提高的产率和质量的标题衍生物。此外，该方法提供具有良好稳定性的标题化合物。

5. 发明申请

WO2007003982A1 IMPROVED PROCESS FOR THE MANUFACTURE OF FLECAINIDE 审中-公开
标题翻译：改善弗莱卡宁制造工艺
公开(公告)号：WO2007003982A1
公开(公告)日：2007-01-11
申请号：PCT/IB2005/002682
申请日：2005-09-09
申请人： GLADE ORGANICS PRIVATE LIMITED , CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, shankar , LIMBAD, Piyush, Bhikhubhai , JHA, Rajesh, Jagannathbhai , JOSHI, Vipul, Narbheshankar
发明人： CHAWLA, Harmander, Pal, Singh , CHOWDHARY, Anil, shankar , LIMBAD, Piyush, Bhikhubhai , JHA, Rajesh, Jagannathbhai , JOSHI, Vipul, Narbheshankar
IPC分类号： C07D213/127 , C07D213/40
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。然后将得到的混合酸酐与2-氨基甲基吡啶在-10至-40℃下冷凝，水后处理得到的产物通过结晶纯化。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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