Merck Sharp + Dohme Corp.

Zhejiang Huahai Pharmaceutical Co., Ltd.

Shanghai Syncores Technologies Inc. Ltd.

Jinfeng Yao

Bin Hu

Philip E Sanderson

Richard Soll

Jiabing Wang

Luning Huang

Mingxiang Cui

Boyu Wang

Zhifa Pu

Jeannie Zhang

Hongjie Zhang

Qi Chen

Shuangxi Hu

Xue Tang

Yongjin Yan

The invention relates to a method for synthesizing an intermediate of Apixaban comprising reacting a compound of formula I with 5-chloro-valeryl chloride in the presence of inorganic base in an inert solvent to obtain a compound of formula II, with the reaction formula of (A), wherein R is selected from nitro group and the group (B). The method is mild in reaction condition, simple in operation, easy in purification, inexpensive in production cost, environmental-friendly, and suitable for industrial production. 

Method for synthesizing key intermediate of apixaban

The instant invention provides for substituted fused pyrimidine compounds of Formula A that inhibit Akt activity: In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Inhibitors of AKT activity

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Shanghai, China

Jinfeng Yao