PREPARATION OF PAROXETINE INVOLVING NOVEL INTERMEDIATES
    5.
    发明公开
    PREPARATION OF PAROXETINE INVOLVING NOVEL INTERMEDIATES 审中-公开
    法制备的新的中间体帕罗西汀

    公开(公告)号:EP1482939A4

    公开(公告)日:2005-10-12

    申请号:EP02729099

    申请日:2002-05-01

    申请人: TEVA PHARMA

    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 SOCl 2 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.