Invention Grant
- Patent Title: Process for preparing ibrutinib and its intermediates
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Application No.: US15336418Application Date: 2016-10-27
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Publication No.: US09834561B2Publication Date: 2017-12-05
- Inventor: Tsung-Yu Hsiao , MengFen Ho , HsinChang Tseng , WenShing Tsao , YuanChang Huang , Wei-Shuo Lo
- Applicant: SCINOPHARM TAIWAN, LTD.
- Applicant Address: TW Tainan
- Assignee: SCINOPHARM TAIWAN, LTD.
- Current Assignee: SCINOPHARM TAIWAN, LTD.
- Current Assignee Address: TW Tainan
- Agency: Mintz Levin Cohn Ferris Glovsky and Popeo, P.C.
- Main IPC: A01N43/90
- IPC: A01N43/90 ; A61K31/519 ; C07D487/00 ; C07D487/04 ; C07F9/6561 ; C07D401/04

Abstract:
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.
Public/Granted literature
- US20170145017A1 PROCESS FOR PREPARING IBRUTINIB AND ITS INTERMEDIATES Public/Granted day:2017-05-25
Information query
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