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Synthesis and use of focal adhesion kinase inhibitors
专利权人:
VERASTEM INC
发明人:
CONNIE L. SUN,BEHRENS CARL HENRY,LEI YIXIONG,LI HUI-YIN
申请号:
NZ60480111
公开号:
NZ604801A
申请日:
2011.06.28
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
The disclosure relates to a method of synthesizing a class of inhibitor of Focal Adhesion Kinase (FAK) of formula (I), wherein the variables are as defined in the speicifcation, 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. These FAK-inhibitory compounds of formula (I) are suitable for the treatment of inflammatory and immune disorders and for the treatment of arthritis.
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