Preparation method of nemategravir intermediate

The invention belongs to the field of medicinal chemistry, and particularly relates to a preparation method of a nemategravir key intermediate as shown in a formula I and a method for synthesizing high-purity nemategravir by using the intermediate. Compared with the prior art, the nemategravir inter...

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Bibliographische Detailangaben
Hauptverfasser: YANG ZHANXIONG, CHEN XIANGFENG, ZHANG MANMAN, SONG HAITAO, QIU HAIZHEN, TIAN SHUAIHUA
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the field of medicinal chemistry, and particularly relates to a preparation method of a nemategravir key intermediate as shown in a formula I and a method for synthesizing high-purity nemategravir by using the intermediate. Compared with the prior art, the nemategravir intermediate shown in the formula I is prepared by removing the Boc protecting group through trifluoroacetic acid, a nemategravir crude product obtained through follow-up reaction is high in purity, various isomers are not detected, the overall yield can reach 45%, the production cost is greatly reduced, and industrial production is facilitated. 本发明属于药物化学领域,具体涉及一种式I所示的奈玛特韦关键中间体的制备方法以及利用该中间体合成高纯度奈玛特韦的方法。与现有技术相比,本发明采用三氟乙酸脱除Boc保护基制得式I所示的奈玛特韦中间体,经过后续反应获得的奈玛特韦粗品纯度高,各种异构体均未检出,整体收率可达到45%,生产成本大幅降低,便于工业化生产。