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11. 发明授权

US06956121B2 Preparation of paroxetine involving novel intermediates 失效
公开(公告)号：US06956121B2
公开(公告)日：2005-10-18
申请号：US10137087
申请日：2002-05-01
申请人： Gideon Pilarski , Ilya Avrutov
发明人： Gideon Pilarski , Ilya Avrutov
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： Disclosed are processes for preparing novel carbamate intermediates of paroxetine comprising dealkylating N-alkylparoxetine by reaction thereof with a haloalkyl ester of a haloformic acid, in a suitable organic solvent. Also disclosed are processes for preparing paroxetine comprising hydrolyzing the novel carbamate intermediates in a suitable solvent. Paroxetine prepared by the above processes can be neutralized with hydrogen chloride and crystallized as paroxetine hydrochloride anhydrous, hemihydrate or as a solvate of isopropanol. The invention is further directed to the novel carbamate intermediates formed by the disclosed processes.

12. 发明授权

US08258322B2 Synthesis of hexahydrodibenzopyranones 失效
标题翻译：六氢二苯并吡喃酮的合成
公开(公告)号：US08258322B2
公开(公告)日：2012-09-04
申请号：US12549919
申请日：2009-08-28
申请人： Valeriy Mikaylo , Subakar Paramanantham , Ilya Avrutov , Martyn A. Brown , Zemin Li , Natalie Lazarowych
发明人： Valeriy Mikaylo , Subakar Paramanantham , Ilya Avrutov , Martyn A. Brown , Zemin Li , Natalie Lazarowych
IPC分类号： C07D311/80
CPC分类号： C07D311/80
摘要： An improved process is provided for the synthesis of hexahydrodibenzo[b,d]pyran-9-ones, such as nabilone.
摘要翻译：提供了六氢二苯并[b，d]吡喃-9-酮如奈匹酮的合成方法。

13. 发明授权

US06930186B2 Process for the preparation of paroxetine substantially free of alkoxy impurities 失效
公开(公告)号：US06930186B2
公开(公告)日：2005-08-16
申请号：US10170709
申请日：2002-06-13
申请人： Valerie Niddam , Ilya Avrutov
发明人： Valerie Niddam , Ilya Avrutov
IPC分类号： C07D211/22 , C07D405/12 , C07D407/12
CPC分类号： C07D405/12 , C07D211/22
摘要： The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities. The alkoxy impurity is reacted with an ether cleaving agent to generate the corresponding phenol, which is separated, yielding the desired product substantially free of alkoxy impurities. Paroxetine intermediates such as PMA, paroxetine, and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities also form part of the present invention.

14. 发明申请

US20050277669A1 Preparation of paroxetine involving novel intermediates 审中-公开
标题翻译：涉及新中间体的帕罗西汀的制备
公开(公告)号：US20050277669A1
公开(公告)日：2005-12-15
申请号：US11206351
申请日：2005-08-17
申请人： Gideon Pilarski , Ilya Avrutov
发明人： Gideon Pilarski , Ilya Avrutov
IPC分类号： C07D405/12 , A61K31/452 , C07D47/02
CPC分类号： C07D405/12
摘要： Disclosed are processes for preparing novel carbamate intermediates of paroxetine comprising dealkylating N-alkylparoxetine by reaction thereof with a haloalkyl ester of a haloformic acid, in a suitable organic solvent. Also disclosed are processes for preparing paroxetine comprising hydrolyzing the novel carbamate intermediates in a suitable solvent. Paroxetine prepared by the above processes can be neutralized with hydrogen chloride and crystallized as paroxetine hydrochloride anhydrous, hemihydrate or as a solvate of isopropanol. The invention is further directed to the novel carbamate intermediates formed by the disclosed processes.
摘要翻译：公开了制备帕罗西汀的新型氨基甲酸酯中间体的方法，其包括在合适的有机溶剂中通过与卤代甲酸的卤代烷基酯反应将N-烷基帕罗西汀脱烷基化。还公开了制备帕罗西汀的方法，包括在合适的溶剂中水解新的氨基甲酸酯中间体。通过上述方法制备的帕罗西汀可以用氯化氢中和，并以无水的帕罗西汀盐酸盐，半水合物或异丙醇的溶剂化物的形式结晶。本发明还涉及由所公开的方法形成的新的氨基甲酸酯中间体。

15. 发明授权

US06723855B2 Method for synthesizing leflunomide 失效
标题翻译：合成来氟米特的方法
公开(公告)号：US06723855B2
公开(公告)日：2004-04-20
申请号：US09779928
申请日：2001-02-08
申请人： Ilya Avrutov , Neomi Gershon , Anita Liberman
发明人： Ilya Avrutov , Neomi Gershon , Anita Liberman
IPC分类号： C07D26118
CPC分类号： C07D261/18 , A61K31/42
摘要： A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided in which the carboxylic acid group of 5-methylisoxazole-4-carboxylic acid is chlorinated, forming 5-methylisoxazole-4-carboxylic acid chloride. The acid chloride is then reacted without intermediate distillation with 4-trifluoromethylaniline in the presence of an alkali metal or alkaline-earth metal bicarbonate acid scavenger.
摘要翻译：提供了从5-甲基异恶唑-4-羧酸和4-三氟甲基苯胺合成来氟米特的方法，其中将5-甲基异恶唑-4-羧酸的羧酸基团氯化，形成5-甲基异恶唑-4-甲酰氯。然后在碱金属或碱土金属碳酸氢盐清除剂的存在下，将酰氯与4-三氟甲基苯胺进行中间蒸馏反应。

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