| 发明名称 |
PROCESS FOR PREPARING CINACALCET HYDROCHLORIDE |
| 摘要 |
Method for preparing cinacalcet hydrochloride having the steps of heating (R)-1-naphthyl ethylamine (Formula I) and 3-(trifluoromethyl)benzene (Formula II);;wherein L is a halogen atom, methanesulfonate group (OMs), p-Toluenesulfonate (OTs), or triflate (OTf), in an organic solvent in presence of an inorganic base, refluxing until 3-(trifluoromethyl)benzene is completely consumed, obtaining a reaction mixture containing cinacalcet, and after treatment, obtaining cinacalcet hydrochloride having a formula of;;The post treatment separates (R)-1-naphthyl ethylamine hydrochloride and cinacalcet hydrochloride by adjusting pH value, extraction, and other simple operations, and the (R)-1-naphthyl ethylamine obtained is recycled for preparing the next batch of cinacalcet hydrochloride. |
| 申请公布号 |
US2015080608(A1) |
申请公布日期 |
2015.03.19 |
| 申请号 |
US201414556026 |
申请日期 |
2014.11.28 |
| 申请人 |
Shanghai Jingxin Biomedical Co., Ltd. ;Shangyu Jingxin Pharmaceutical Co., Ltd. |
发明人 |
XU Miaohuan;Huang Yue;Zhang Min |
| 分类号 |
C07C209/02 |
主分类号 |
C07C209/02 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
1. A process for preparing cinacalcet hydrochloride, comprising
charging (R)-1-naphthyl ethylamine (Formula I) and 3-(trifluoromethyl) benzene compound (Formula II)at a molar ratio of (1.0-5.0):1 in a suitable organic solvent,
heating and refluxing until the 3-(trifluoromethyl) benzene compound is completely consumed in presence of an inorganic base, obtaining a mixture containing cinacalcet, and obtaining cinacalcet hydrochloride having a formula offrom the mixture containing cinacalcet after acidification with hydrochloride and extraction,
wherein L in Formula II is a halogen, methanesulfonate, p-Toluenesulfonate, or triflate. |
| 地址 |
Shanghai CN |
