发明名称 Process for the preparation of fesoterodine or a salt thereof
摘要 A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having low content in impurities.
申请公布号 US8772340(B2) 申请公布日期 2014.07.08
申请号 US201113295224 申请日期 2011.11.14
申请人 Dipharma Francis S.r.l. 发明人 Artico Marco;Attolino Emanuele;Allegrini Pietro;Razzetti Gabriele
分类号 A61K31/216;A61K31/225;C07C69/34 主分类号 A61K31/216
代理机构 Rothwell, Figg, Ernst & Manbeck, P.C. 代理人 Rothwell, Figg, Ernst & Manbeck, P.C.
主权项 1. A process for the preparation of Fesoterodine of formula (I), or a pharmaceutically acceptable salt thereofcomprising the selective esterification of the phenolic hydroxyl of a compound of formula (II)wherein the selective esterification comprises the reaction of a compound of formula (II) with an acylating agent, in the presence of an alcoholic solvent and a base, wherein said alcoholic solvent is a C1-C2 alkanol, a mixture of C1-C2 alkanols or a mixture of a C1-C2 alkanol with an inert solvent.
地址 Baranzate (MI) IT