发明名称 Process for the preparation of ospemifene
摘要 The present invention is related to the process for the preparation ospemifene or (Z)-2-[4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy]ethanol (I) and to intermediate compounds used in the process.;
申请公布号 US9321712(B2) 申请公布日期 2016.04.26
申请号 US201314436706 申请日期 2013.10.17
申请人 FERMION OY 发明人 Tois Jan;Pihko Ainoliisa;Grumann Arne
分类号 C07C41/26;C07C69/24;C07C67/14;C07C67/293;C07C67/297;C07C69/28;C07C69/753;C07C69/76 主分类号 C07C41/26
代理机构 Oblon, McClelland, Maier & Neustadt, L.L.P. 代理人 Oblon, McClelland, Maier & Neustadt, L.L.P.
主权项 1. A process of preparing a compound of formula (I) which process comprises (a) reacting a compound of formula (III)  wherein R is a protecting group tolerant to Grignard or other organometallic reagents, with phenylmagnesium halide, thereby obtaining a compound of formula (IV) wherein R is as defined in formula (III), (b) treating the compound of formula (IV) with hydrochloric acid, thereby obtaining a compound of formula (V) wherein R is as defined as in formula (III), and (c) cleaving the ester bond of the compound of formula (V), thereby obtaining the compound of formula (I).
地址 Espoo FI