A process for the preparation of resmetiromide and intermediates thereof

By carrying out a nucleophilic substitution reaction and hydrolysis of compound I with silanol in an aprotic organic solvent, combined with pH adjustment for crystallization, the problem of easy cleavage of diphenyl ether bonds at high temperatures was solved, and the preparation of high-purity, high-yield resimetiro intermediates was achieved, simplifying the operation process and reducing environmental pollution.

CN122404233APending Publication Date: 2026-07-17AURISCO PHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-06-15
Publication Date
2026-07-17

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Abstract

本发明提供了一种瑞司美替罗及其中间体，化合物II的制备方法。化合物II的制备方法包括步骤：化合物I与硅醇盐进行亲核取代反应，得到的中间体进行水解，生成化合物II，反应式如下。本发明的制备方法的反应条件温和，反应速度快，后处理简单，且得到的产物中杂质少。，其中R4选自H或者氨基保护基,R5选自H或者异丙基。
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