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PROCESS FOR PREPARING IBRUTINIB AND ITS INTERMEDIATES
专利权人:
发明人:
申请号:
EP16860399.1
公开号:
EP3368537A1
申请日:
2016.10.28
申请国别(地区):
EP
年份:
2018
代理人:
摘要:
The present invention provides efficient, economical, and improved methods for synthesizing ibrutinib and intermediates thereof. The invention involves a unique biphasic acylation reaction system which advantageously allows for easy separation of ibrutinib from the reaction mixture without additional extraction and wash steps. The isolated ibrutinib formed using the methods described herein can be useful in the preparation of an amorphous form of ibrutinib. In some embodiments, the isolated ibrutinib produced by the processes described herein is a homogenous solution of ibrutinib and DMSO which may be directly used in the formation of the amorphous polymorph. In some embodiments, the isolated ibrutinib is solid ibrutinib. The solid ibrutinib may also be used in the formation of amorphous ibrutinib.
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