Invention Grant
- Patent Title: Method for preparing epirubicin and intermediate thereof
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Application No.: US14900921Application Date: 2013-07-02
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Publication No.: US09963479B2Publication Date: 2018-05-08
- Inventor: Wei Yan , Wanzeng Tong , Jianping Wang , Weiqiang Yang , Hongguan Qian
- Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
- Applicant Address: CN
- Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
- Current Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
- Current Assignee Address: CN
- Agency: Lerner, David, Littenberg. Krumholz & Mentlik, LLP
- International Application: PCT/CN2013/078672 WO 20130702
- International Announcement: WO2015/000132 WO 20150108
- Main IPC: C07H15/252
- IPC: C07H15/252

Abstract:
The present invention provides a method for preparing epirubicin and an intermediate adaptive to the method. The preparation method may include: reacting tert-Butyldimethylsilyl chloride with N-trifluoroacetyl adriamycin to obtain a compound of formula I N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl adriamycin; oxidizing the compound of formula I to obtain a compound of formula II 4′-ketone-N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl adriamycin; reducing the compound of formula II to obtain a compound of formula III N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl epirubicin; and performing deprotection and hydrolysis reactions on the compound of formula III to obtain epirubicin. The method of the present invention needs low cost, fewer reaction steps, provides high yield and high product purity, and avoids serious pollution caused by a bromination reaction in a conventional method.
Public/Granted literature
- US20160137683A1 Method for Preparing Epirubicin and Intermediate Thereof Public/Granted day:2016-05-19
Information query
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