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1. 发明申请

US20060128812A1 Process for the preparation of 2-[(diphenylmethyl) thio] acetamide 失效
标题翻译：制备2 - [（二苯基甲基）硫代]乙酰胺的方法
公开(公告)号：US20060128812A1
公开(公告)日：2006-06-15
申请号：US10543748
申请日：2004-01-30
申请人： Surendra Bhatt , Jiten Patel , Dinesh Panchasara , Hetal Shah , Keshav Deo , Vinod Kansal
发明人： Surendra Bhatt , Jiten Patel , Dinesh Panchasara , Hetal Shah , Keshav Deo , Vinod Kansal
IPC分类号： A61K31/165 , C07C315/02
CPC分类号： C07C319/20 , C07C315/02 , C07C323/52 , C07C323/60 , C07C317/44
摘要： Process for the preparation of 2-[(diphenylmethyl)thioacetamide, an intermediate for the preparation of Modafinil which is a CNS stimulant and used for the treatment of narcolepsia. The process comprises reacting 2-[(diphenylmethyl)thio]acetic acid with alcohols, in presence of catalytic amount of inorganic acid or organic acid at reflux temperature of alcohol to obtain corresponding ester which is reacted with ammonia to give 2-[(diphenylmethyl)thio]acetamide. If desired 2-[(diphenylmethyl)thioacetamide thus produced is reacted with hydrogen peroxide to produce Modafinil.
摘要翻译：制备2 - [（二苯基甲基）硫代乙酰胺的方法，用于制备作为CNS兴奋剂的莫达非尼的中间体，用于治疗发作性睡病。该方法包括在催化量的无机酸或有机酸的存在下，在醇的回流温度下使2 - [（二苯基甲基）硫代]乙酸与醇反应，得到相应的与氨反应的酯，得到2 - [（二苯基甲基）硫代]乙酰胺。如果需要，将如此制备的2 - [（二苯基甲基）硫代乙酰胺与过氧化氢反应以产生莫达非尼。

2. 发明授权

US07186860B2 Process for the preparation of 2-[(diphenylmethyl) thio] acetamide 失效
标题翻译：制备2 - [（二苯基甲基）硫代]乙酰胺的方法
公开(公告)号：US07186860B2
公开(公告)日：2007-03-06
申请号：US10543748
申请日：2004-01-30
申请人： Surendra B. Bhatt , Jiten R. Patel , Dinesh Panchasara , Hetal R. Shah , Keshav Deo , Vinod Kumar Kansal
发明人： Surendra B. Bhatt , Jiten R. Patel , Dinesh Panchasara , Hetal R. Shah , Keshav Deo , Vinod Kumar Kansal
IPC分类号： C07C323/29
CPC分类号： C07C319/20 , C07C315/02 , C07C323/52 , C07C323/60 , C07C317/44
摘要： Process for the preparation of 2-[(diphenylmethyl)thioacetamide, an intermediate for the preparation of Modafinil which is a CNS stimulant and used for the treatment of narcolepsia. The process comprises reacting 2-[(diphenylmethyl)thio]acetic acid with alcohols, in presence of catalytic amount of inorganic acid or organic acid at reflux temperature of alcohol to obtain corresponding ester which is reacted with ammonia to give 2-[(diphenylmethyl)thio]acetamide. If desired 2-[(diphenylmethyl)thioacetamide thus produced is reacted with hydrogen peroxide to produce Modafinil.
摘要翻译：制备2 - [（二苯基甲基）硫代乙酰胺的方法，用于制备作为CNS兴奋剂的莫达非尼的中间体，用于治疗发作性睡病。该方法包括在催化量的无机酸或有机酸的存在下，在醇的回流温度下使2 - [（二苯基甲基）硫代]乙酸与醇反应，得到相应的与氨反应的酯，得到2 - [（二苯基甲基）硫代]乙酰胺。如果需要，将如此制备的2 - [（二苯基甲基）硫代乙酰胺与过氧化氢反应以产生莫达非尼。

3. 发明申请

US20070265457A1 Process for Lactonization in the Preparation of Statins 失效
标题翻译：在制备他汀类药物中的乳化过程
公开(公告)号：US20070265457A1
公开(公告)日：2007-11-15
申请号：US11574872
申请日：2004-09-08
申请人： Govind Singh , Paramvir Bhadwal , Sanjay Jaiswal , Dinesh Panchasara , Rajesh Thaper , Sushil Dubey , Jag Khanna
发明人： Govind Singh , Paramvir Bhadwal , Sanjay Jaiswal , Dinesh Panchasara , Rajesh Thaper , Sushil Dubey , Jag Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： The present invention relates to an improved and industrial friendly process for lactonization to produce compound of the Formula [I], from compound of the Formula [II] in presence of an inorganic compound as a suitable lactonizing agent, preferably alkali metal hydrogen sulfate, and crystallizing the obtained lactone product in a solvent; or treating compound of the Formula [II] in the presence of an inorganic compound preferably alkali metal hydrogen sulfate using phase transfer catalyst in heterogeneous phase followed by crystallizing the obtained lactone product in a solvent.
摘要翻译：本发明涉及在无机化合物作为合适的内酯化剂，优选碱金属硫酸氢盐的存在下，通过式[II]的化合物制备式[I]的化合物的内酯化的改进和工业友好的方法，以及将所得内酯产物在溶剂中结晶; 或在无机化合物（优选碱金属硫酸氢盐）存在下处理式[II]化合物，使用非均相相转移催化剂，然后将所得内酯产物在溶剂中结晶。

4. 发明申请

US20100317849A1 Process For Producing Pure And Stable Form Of 2-Methyl-4-(4-Methyl-1-Piperazinyl) -10H-Thieno[2,3-B] [1,5] Benzodiazepine 审中-公开
标题翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂的纯稳定形式的制备方法
公开(公告)号：US20100317849A1
公开(公告)日：2010-12-16
申请号：US12225080
申请日：2006-03-14
申请人： Dinesh Panchasara , Poorvi Gupta , Geetesh Kaushik , Sushil Dubey
发明人： Dinesh Panchasara , Poorvi Gupta , Geetesh Kaushik , Sushil Dubey
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Disclosed is an improved process for producing pure and thermally color stable crystalline Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine and product thereof. The process comprises of reacting 2-(2-aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][l,5J benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine in a mixture of solvents. Further the invention also provides a new polymorph of Olanzapine, dihydrate Form Ji and process for its preparation and a new hydrate Form J2 of Olanzapine having moisture content 1-3% and process for its preparation.
摘要翻译：公开了一种改进的2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和产物的纯色和热色稳定晶型I的方法其中。该方法包括使2-（2-氨基苯胺基）-5-甲基噻吩-3-腈与N-甲基哌嗪与N-甲基哌嗪酸盐一起反应，得到2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂。还公开了通过将粗2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂的粗2- -4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂在溶剂混合物中。此外，本发明还提供了奥氮平，二水合物形式及其制备方法和水分含量为1-3％的奥氮平新型水合物形式J2的新型多晶型物及其制备方法。

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