SYNTHESIS PROCESS OF RUXOLITINIB

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compo...

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Bibliographische Detailangaben
Hauptverfasser: Yao, Huadong, Wang, Hubo, Zhou, Zhou, Zhu, Xueyan, Yang, Leilei, Zhang, Xiquan, Zhang, Aiming
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.