Verastem, Inc.

Yixiong Lei

Hui-Yin Li

Carl Henry Behrens

Connie L Sun

An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.

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Newark, DE, United States of America

Yixiong Lei