| 发明名称 | Process for the preparation of bazedoxifene acetate and intermediates thereof | ||
| 摘要 | A novel process is described for the preparation of pharmaceutically useful compounds such as 1-{4-[2-(azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate of the formula-1 using 2-(4-{[5-(benzyloxy)-2-[4-(benzyloxy)phenyl]-3-methyl-1H-indol-1-yl]methyl}phenoxy)ethyl-4-methylbenzenzene-1-sulfonate (formula 2a).; | ||
| 申请公布号 | US8889896(B2) | 申请公布日期 | 2014.11.18 |
| 申请号 | US201313908194 | 申请日期 | 2013.06.03 |
| 申请人 | Divi's Laboratories, Ltd. | 发明人 | Divi Murali Krishna Prasad;Padakandla Gundu Rao;Rao Bolneni Nageswara;Suresh Dandu Venkata |
| 分类号 | C07C303/00;C07C301/00;C07C309/75;C07D209/12;C07C303/28;C07C303/30 | 主分类号 | C07C303/00 |
| 代理机构 | Caesar, Rivise, Bernstein, Cohen & Pokotilow, Ltd. | 代理人 | Caesar, Rivise, Bernstein, Cohen & Pokotilow, Ltd. |
| 主权项 | 1. A process for the preparation of a sulfonic acid ester of 2-(4-bromomethyl)phenoxy ethanol (formula 18) useful as an intermediate in the preparation of 1-{4-[2-(azepan-1-1)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol comprising (a) treating 4-(2-hydroxyethyloxy)benzaldehyde (formula 15) with the sulphonic acid chloride in a dichloromethane solvent and a triethylamine organic base and after suitable work up isolate the sulphonic acid ester (formula 16), (b) treating the ester so obtained with a metal hydride reducing agent, in a suitable solvent to obtain the sulphonic acid ester of 2-(4-hydroxymethyl) phenoxy ethanol (formula 17), (c) reacting the product so obtained from step (b) with phosphorus tribromide in dichloromethane and after suitable work up isolating the sulfonic acid ester of 2-(4-bromomethyl)phenoxy ethanol (formula 18), | ||
| 地址 | IN | ||