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IMPROVED PROCESS FOR THE PREPARATION OF RIZATRIPTAN BENZOATE

机译:苯甲酸利扎曲普坦的制备工艺得到改进

摘要

Present invention discloses an improved and commercially viable process for the preparation of rizatriptan benzoate of formula-I. According to the present process the hydrazone intermediate derived from the phenylhydrazine of formula-Ill and 4-dimethylaminobutyraldehyde diethyl acetal is gradually heated to 60-70°C in aqueous sulfuric acid medium and maintained for 3-4hr to get rizatriptan with less dimeric impurity of formula-X. The resultant rizatriptan is isolated and converted into the pharmaceutical^ acceptable benzoate salt. Present process produces less percentage of dimeric (less than 3%) or polymeric impurities compared to the prior art process and more yield of rizatriptan. Rizatriptan benzoate produced according to the present process has more than 99.5% purity with less than 0.1% dimeric impurity of formula-X by HPLC. Rizatriptan benzoate is useful for the treatment of migraine.
机译:本发明公开了制备式I的利扎曲普坦苯甲酸酯的改进的且商业上可行的方法。根据本方法,将衍生自式III的苯基肼和4-二甲基氨基丁醛二乙基乙缩醛的中间体在硫酸水溶液中逐渐加热至60-70℃,并保持3-4小时,得到具有较少二聚体杂质的利扎曲普坦。公式-X。分离得到的利扎曲普坦,并将其转化为药学上可接受的苯甲酸盐。与现有技术的方法相比,本发明的方法产生较少百分比的二聚体(小于3%)或聚合物杂质,并且利扎曲普坦的产率更高。根据本方法生产的利扎曲普坦苯甲酸酯具有超过99.5%的纯度,通过HPLC,具有小于0.1%的式-X的二聚体杂质。利扎曲普坦苯甲酸酯可用于治疗偏头痛。

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