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公开(公告)号：EP1015428A1
公开(公告)日：2000-07-05
申请号：EP98946097.7
申请日：1998-09-17
IPC分类号： C07D207/416
CPC分类号： C07C303/22 , C07C309/17 , C07D207/416
摘要： The salt of a sulfonated succinic acid is cyclized, then converted to novel sulfonated hydroxamic acids by reaction with hydroxylamine (which is added or formed in situ), and the novel hydroxamic acid is then cyclized to the sulfo-N-hydroxysuccinimide salt. Novel sulfo-hydroxamic acid intermediates are formed during this procedure. A process of forming a sulfo-N-hydroxysuccinimide by cyclizing a sulfohydroxamic acid is also described. Alternatively, the present invention describes a novel method for the synthesis of sulfo-N-hydroxysuccinimide salts in which commercially available sulfosuccinic acid salt in an aqueous medium is heated in the presence of an alcohol to form a diester of the succinic acid sulfonate. The diester is then reacted with hydroxylamine (e.g., from the hydrochloride salt) (e.g., in an alkaline buffered aqueous environment, e.g., at room temperature) to form the sulfo-N-hydroxysuccinimide. This is an extremely simple and direct process that does not produce a significant level of irremovable impurities.
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公开(公告)号：EP1015428B1
公开(公告)日：2003-05-02
申请号：EP98946097.7
申请日：1998-09-17
IPC分类号： C07D207/416
CPC分类号： C07C303/22 , C07C309/17 , C07D207/416
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