首页> 外国专利> Preparing diacerein useful to treat e.g. psoriasis, comprises oxidizing aloe-emodin to obtain rhein, preparing rhein diacyl derivative, optionally purifying and hydrolyzing rhein diacyl derivative, and acetylating the rhein to diacerein

Preparing diacerein useful to treat e.g. psoriasis, comprises oxidizing aloe-emodin to obtain rhein, preparing rhein diacyl derivative, optionally purifying and hydrolyzing rhein diacyl derivative, and acetylating the rhein to diacerein

机译:制备双醋瑞因可用于治疗例如牛皮癣包括氧化芦荟大黄素以获得大黄酸,制备大黄酸二酰基衍生物,任选地纯化和水解大黄酸二酰基衍生物,以及将大黄酸乙酰化为双醋瑞因。

摘要

Preparation of diacerein comprises oxidizing aloe-emodin to obtain rhein, preparing rhein diacyl derivative, optionally, purifying and hydrolyzing the rhein diacyl derivative, and acetylating the rhein to diacerein. Independent claims are included for: (1) a process for purifying rhein diacyl derivative comprising dissolving the rhein diacyl derivative in tetrahydrofuran, contacting with toluene and isolating the diacyl rhein; (2) a process for purification of diacerein comprising dissolving the diacerein in N-methyl-pyrrolidone, where the dissolving is carried out at a high temperature, adding alcohol and/or water, cooling the solution at ambient temperature, and isolating the diacerein under solid product form; and (3) a dipropionyl rhein and their salts, as an intermediate product in the synthesis of diacerein. ACTIVITY : Antiarthritic; Antirheumatic; Antipsoriatic. MECHANISM OF ACTION : None given.
机译:双醋瑞因的制备包括氧化芦荟大黄素以获得大黄酸,制备大黄酸二酰基衍生物,任选地,纯化和水解大黄酸二酰基衍生物,并将大黄酸乙酰化为双醋瑞因。包括以下独立权利要求:(1)纯化大黄酸二酰基衍生物的方法,该方法包括将大黄酸二酰基衍生物溶解在四氢呋喃中,与甲苯接触并分离出二酰基大黄酸。 (2)双醋瑞因的纯化方法,包括将双醋瑞因溶解在N-甲基-吡咯烷酮中,其中溶解在高温下进行,加入醇和/或水,在室温下冷却该溶液,并在室温下分离双醋瑞因。固体产品形式; (3)作为双醋瑞因合成中的中间产物的二丙酰基大黄酸及其盐。活动:抗关节炎;抗风湿;对牛皮癣。作用机理:未给出。

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