Invention Grant
- Patent Title: Preparation process for high-purity dabigatran etexilate
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Application No.: US16301769Application Date: 2017-05-24
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Publication No.: US10538507B2Publication Date: 2020-01-21
- Inventor: Lingjie Chen , Wenling Zhang , Peng Wang
- Applicant: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD , ZHEJIANG HUAHAI ZHICHENG PHARMACEUTICAL CO., LTD.
- Applicant Address: CN Taizhou CN Linhai
- Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD,ZHEJIANG HUAHAI ZHICHENG PHARMACEUTICAL CO., LTD.
- Current Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD,ZHEJIANG HUAHAI ZHICHENG PHARMACEUTICAL CO., LTD.
- Current Assignee Address: CN Taizhou CN Linhai
- Agency: Norton Rose Fulbright US LLP
- Priority: CN201610347598 20160524
- International Application: PCT/CN2017/085750 WO 20170524
- International Announcement: WO2017/202341 WO 20171130
- Main IPC: C07D235/04
- IPC: C07D235/04 ; C07D401/12 ; B01D9/00

Abstract:
Provided is a purifying method for dabigatran etexilate free base, comprising subjecting a dabigatran etexilate free base crude product to water slurrying to obtain a crude product B; then conducting recrystallization on the crude product B with acetone and water to obtain a crude product C; and subsequently, purifying the crude product C with a mixed solvent of tetrahydrofuran and ethyl acetate, filtering and drying to obtain a dabigatran etexilate free base finished product. The purifying method of the present invention can effectively remove various impurities and is suitable for workshop production. Salts and water-soluble organic impurities are removed by purified water slurrying, impurities with a high polarity are removed by purifying with an acetone-water solution, and impurities with a low polarity are removed by purifying with a mixed solvent of tetrahydrofuran and ethyl acetate.
Public/Granted literature
- US20190152945A1 PREPARATION PROCESS FOR HIGH-PURITY DABIGATRAN ETEXILATE Public/Granted day:2019-05-23
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