Invention Grant
- Patent Title: Method for preparing Ibrutinib
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Application No.: US15159600Application Date: 2016-05-19
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Publication No.: US09598425B2Publication Date: 2017-03-21
- Inventor: Xuenong Xu
- Applicant: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
- Applicant Address: CN Suzhou
- Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
- Current Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
- Current Assignee Address: CN Suzhou
- Agency: Perkins Coie LLP
- Priority: CN201310589969 20131120
- Main IPC: C07D487/00
- IPC: C07D487/00 ; C07D487/04

Abstract:
Provided is a method for preparing Ibrutibin (I), and steps of preparing same comprise: 4-benzyloxybenzoyl chloride (II) is used as a raw material, condensation and methoxidation reactions occur among 4-benzyloxybenzoyl chloride (II), malononitrile, and dimethyl sulfate to generate 4-benzyloxyphenyl(methoxy)vinylidenedicyanomethane (III), pyrazole cyclization occurs between the intermediate (III) and 1-(3R-hydrazino-1-piperidino)-2-propylene-1-ketone (IV) to acquire 1-[(3R)-[3-(4-benzyloxyphenyl)-4-nitrile-5-amino-1H-pyrazole]-1-piperidino]-2 propylene-1-ketone (V), and pyrimidine cyclization occurs between an intermediate (V) and a cyclizing agent to prepare Ibrutinib (I). In the preparation method, the raw material is readily available, and the process is simple, economical, environmentally friendly, and is suitable for industrial production.
Public/Granted literature
- US20160264584A1 Method for Preparing Ibrutinib Public/Granted day:2016-09-15
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