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