Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Lianyungang Runzhong Pharmaceutical Co., Ltd.

Shanghai Dude Medical Science and Technology Co., Ltd.

Leilei Yang

Xiquan Zhang

Aiming Zhang

Xin Liu

Xueyan Zhu

Hubo Wang

Xingdong Cheng

Zhou Zhou

Xiaoping Chen

Huadong Yao

Rui Kong

Shan Chen

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. 

Synthesis process of ruxolitinib

The present application relates to a method for preparing Ibutinib as shown by the following synthetic route and the intermediate compounds involved therein. 

Process for preparing ibrutinib

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Leilei Yang