| 发明名称 |
METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE |
| 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. |
| 申请公布号 |
US2015038704(A1) |
申请公布日期 |
2015.02.05 |
| 申请号 |
US201314380875 |
申请日期 |
2013.02.22 |
| 申请人 |
CHINA NATIONAL MEDICINES GUORUI PHARMACEUTICAL CO. LTD. ;SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY |
发明人 |
Zhang Fuli;Liang Bin;Yang Chunbo;Liu Chonghao;Gao Yang;Wang Jian;Jiang Min |
| 分类号 |
C07D413/10 |
主分类号 |
C07D413/10 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
1. A method for preparing Rivaroxaban intermediate I, comprising: in a non-protonic solvent, under the effect of a lewis acid, performing cyclization reaction with compound II and compound III, reaction temperature ranging from 20° C. to 160° C., wherein R is an amino substituted by an amino protecting group. |
| 地址 |
Huianan, Anhui CN |
