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1.发明授权Method for preparing benzisoxazole methane sulfonyl chloride and its amidation to form zonisamide 失效制备苯并异恶唑甲磺酰氯及其酰胺化形成唑尼沙胺的方法公开(公告)号：US06936720B2
公开(公告)日：2005-08-30
申请号：US10373554
申请日：2003-02-24
IPC分类号： A61K31/423 , A61P25/08 , C07B61/00 , C07D261/20 , C07D405/12
CPC分类号： C07D261/20 , C07D405/12
摘要： The present invention relates to a process of preparing benzisoxazole methane sulfonic acid-chloride (BOS—Cl) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also discloses a process of preparing zonisamide via amidation of BOS—Cl. More particularly, the present invention provides a process of preparing zonisamide, comprising the steps of: a) chlorinating BOS, salts or esters thereof, with SOCl2 in an organic solvent and/or in the presence of a catalyst to form BOS—Cl; and b) amidating BOS—Cl in the presence of ammonia selected from the group consisting of aqueous ammonia in a biphasic system, masked ammonia and dry ammonia to form zonisamide.
摘要翻译： 本发明涉及通过苯并异恶唑甲烷磺酸盐的氯化制备苯并异恶唑甲磺酸氯化物（BOS-Cl）作为唑烷酰胺中间体的方法。 本发明还公开了通过BOS-Cl的酰胺化制备唑尼沙胺的方法。 更具体地说，本发明提供了制备唑尼沙胺的方法，包括以下步骤：a）在有机溶剂中和/或在有机溶剂存在下，将BOS，其盐或酯与SOCl 2氯化， 催化剂形成BOS-Cl; 和b）在选自二元体系中的氨水，掩蔽的氨和干氨中的氨存在下使BOS-Cl酰胺化以形成唑尼沙胺。
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公开(公告)号：US20060252770A1
公开(公告)日：2006-11-09
申请号：US11488810
申请日：2006-07-17
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D215/56
摘要： Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.
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公开(公告)号：US20060258674A1
公开(公告)日：2006-11-16
申请号：US11488367
申请日：2006-07-17
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D215/56
摘要： Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.
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公开(公告)号：US20060252771A1
公开(公告)日：2006-11-09
申请号：US11488811
申请日：2006-07-17
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D215/56
摘要： Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.
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公开(公告)号：US20060258676A1
公开(公告)日：2006-11-16
申请号：US11488370
申请日：2006-07-17
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D215/56
摘要： Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.
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6.发明申请公开(公告)号：US20060258675A1
公开(公告)日：2006-11-16
申请号：US11488368
申请日：2006-07-17
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D215/56
摘要： Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.
摘要翻译： 提供加替沙星的新型结晶形式，其中一些是DMSO溶剂合物，以及制备它们的方法。
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