发明名称 |
Method for the preparation of cinacalcet and intermediates and impurities thereof |
摘要 |
A method for the preparation of Cinacalcet is disclosed comprising treating (R)-1-naphthyl ethylamine with an aromatic aldehyde to form (1R)-1-(2-naphthyl)-N-(aryl methylene)ethanamine derivative of Formula (IV), which is further treated with 1-(3-halopropyl)-3-(trifluoromethyl)benzene of Formula (V) to obtain an iminium salt of Formula (VI), followed by hydrolysis to obtain Cinacalcet free base. |
申请公布号 |
US8969623(B2) |
申请公布日期 |
2015.03.03 |
申请号 |
US201314052116 |
申请日期 |
2013.10.11 |
申请人 |
Amneal Pharmaceuticals, LLC |
发明人 |
Mathad Vijayavitthal Thippannachar;Niphade Navnath Chintaman;Shinde Gorakshanath Balasaheb;Ippar Sharad Subhash;Deshmukh Shrikant Prataprao;Panchangam Raghavendra Kumar |
分类号 |
C07C209/00;C07C209/62;C07C209/86;C07C211/08;C07C249/02;C07C251/30;C07C211/30;C07C251/16;C07C251/24;C07C251/06 |
主分类号 |
C07C209/00 |
代理机构 |
Servilla Whitney LLC |
代理人 |
Servilla Whitney LLC |
主权项 |
1. A method of preparing a compound of Formula (I) or a salt thereof, comprising reacting a compound of Formula (IV) with a compound of Formula (V) to produce the compound of Formula (I), wherein Ar is benzyl-, phenyl- or naphthyl-, which may be mono- or di- or poly substituted with alkyl, aryl, alkoxy, amino, hydroxyl, halogen, and nitro groups, and X is chloro, bromo, or iodo. |
地址 |
Bridgewater NJ US |