发明授权
- 专利标题: Method for preparing rivaroxaban intermediate
- 专利标题(中): 制备利伐沙班中间体的方法
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申请号: US14380875申请日: 2013-02-22
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公开(公告)号: US09079892B2公开(公告)日: 2015-07-14
- 发明人: Fuli Zhang , Bin Liang , Chunbo Yang , Chonghao Liu , Yang Gao , Jian Wang , Min Jiang
- 申请人: CHINA NATIONAL MEDICINES GUORUI PHARMACEUTICAL CO., LTD. , SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
- 申请人地址: CN Anhui CN Shanghai
- 专利权人: CHINA NATIONAL MEDICINES GUORUI PHARMACEUTICAL CO., LTD.,SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
- 当前专利权人: CHINA NATIONAL MEDICINES GUORUI PHARMACEUTICAL CO., LTD.,SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
- 当前专利权人地址: CN Anhui CN Shanghai
- 代理机构: Oliff PLC
- 优先权: CN201210044359 20120224
- 国际申请: PCT/CN2013/071769 WO 20130222
- 国际公布: WO2013/123893 WO 20130829
- 主分类号: C07D413/10
- IPC分类号: C07D413/10 ; C07D413/14
摘要:
A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.
公开/授权文献
- US20150038704A1 METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE 公开/授权日:2015-02-05
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