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公开(公告)号：EP4450508A1
公开(公告)日：2024-10-23
申请号：EP21967736.6
申请日：2021-12-17
发明人： MEI, Yijiang , LIU, Shengmin , LI, Yonggang , FAN, Jinmin , HU, Kai , GAO, Shizhao
IPC分类号： C07D513/04 , C07D211/74
摘要： Disclosed are an intermediate of edoxaban tosylate and a preparation method therefor, having the advantages that the preparation process is simple, reaction conditions are mild, the cost is low, and raw materials are easily to be obtained. The method comprises the synthesis steps of: substitution reaction, thiolation reaction, cyclization reaction, esterification reaction with alcohol to obtain a compound represented by formula (V), and then reacting to obtain a compound represented by formula (VI), or directly reacting the compound represented by formula (IV) under the effect of alcohol and acid, to obtain the compound represented by formula (VI), and subjecting the compound represented by formula (VI) to alkali hydrolysis and acid neutralization to obtain a compound represented by formula (VII). The reaction formula is as follows:
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