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    METHOD FOR PREPARING BENZISOXAZOLE METHANE SULFONYL CHLORIDE AND ITS AMIDATION TO FORM ZONISAMIDE
    1.
    发明公开
    METHOD FOR PREPARING BENZISOXAZOLE METHANE SULFONYL CHLORIDE AND ITS AMIDATION TO FORM ZONISAMIDE 审中-公开
    生产工艺BENZISOXAZOLMETHANSULFONYLCHLORID及其酰胺化的教育唑尼沙胺

    公开(公告)号：EP1472236A4

    公开(公告)日：2006-04-19

    申请号：EP03716172

    申请日：2003-02-24

    申请人： TEVA PHARMA ,  TEVA PHARMA

    发明人： MENDELOVICI MARIOARA ,  GERSHON NEOMI ,  NIDAM TAMAR ,  PILARSKI GIDEON ,  STERINBAUM GRETA

    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-CI) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also disloses a process of preparing zonisamide via amidation of BOS-CI. 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： 本发明涉及苯并异恶唑甲磺酸氯化物（BOS-Cl）的制备如经由苯并异恶唑甲磺酸盐的氯化唑尼沙胺中间体的处理。 因此，本发明的盘较少经由BOS-CL的酰胺化制备的唑尼沙胺的方法。 更具体地，本发明提供了制备唑尼沙胺，其包括以下步骤的处理：和/或在一个存在下，在有机溶剂中的）氯化BOS，其盐或酯，具有的SOCl 2 催化剂以形成BOS-CL; 和b）在氨从该组中的两相体系wässrige氨由......组成选择的存在酰胺化BOS-CL，掩蔽的氨和干氨反应形成的唑尼沙胺。

    ZONISAMIDE INTERMEDIATE AND SYNTHESIS
    3.
    发明公开
    ZONISAMIDE INTERMEDIATE AND SYNTHESIS 审中-公开
    ZONISAMID-ZWISCHENPRODUKT UND-SYNTHESE

    公开(公告)号：EP1430037A4

    公开(公告)日：2004-11-17

    申请号：EP02768748

    申请日：2002-08-29

    申请人： TEVA PHARMA

    发明人： NIDAM TAMAR ,  MENDELOVICI MARIOARA ,  SCHWARTZ EDUARD ,  WIZEL SHLOMIT

    IPC分类号： C07D261/20 ,  C07F1/04 ,  C07F3/00 ,  C07F3/04

    CPC分类号： C07D261/20

    摘要： The present invention relates to a novel sulfonation of an intermediate of zonisamide. The sulfonation processes using chlorosulfonic acid as well as acetic anhydride and sulfuric acid in an organic solvent are disclosed. Crystalline forms of benzisoxazole methane sulfonic acid (BOS-H) and its salts (BOS-Na, BOS-Ca, and BOS-Ba) and their novel preparation processes are disclosed.

    摘要翻译： 本发明涉及唑尼沙胺中间体的新型磺化。 公开了在有机溶剂中使用氯磺酸以及乙酸酐和硫酸的磺化方法。 公开了苯并异恶唑甲磺酸（BOS-H）及其盐（BOS-Na，BOS-Ca和BOS-Ba）的结晶形式及其新的制备方法。