发明名称 Process for the preparation of O-desmethyl-venlafaxine and salts thereof
摘要 The present invention relates to a novel process for the preparation of O-desmethyl venlafaxine (ODV) and the pharmaceutically acceptable salts thereof, wherein it comprises (i) provision of spiro-venlafaxine compound as intermediate; (ii) conversion of spiro-venlafaxine intermediate into ODV free base in a one-pot process; and (iii) optionally conversion ODV free base into pharmaceutically acceptable salts. The present invention further relates to novel processes for the preparation of crystalline salts of ODV-succinate and ODV-oxalate.
申请公布号 US8754261(B2) 申请公布日期 2014.06.17
申请号 US200913515871 申请日期 2009.12.16
申请人 Pharmathen S.A. 发明人 Koftis Theoharis V.;Georgopoulou Ioanna;Strongilos Alexandros;Liepouri Fotini;Panagiotidis Theodoros;Lithadioti Alexandra
分类号 C07C211/00 主分类号 C07C211/00
代理机构 AKC Patents 代理人 AKC Patents ;Collins Aliki K.
主权项 1. A process for the preparation of O-desmethyl Venlafaxine, or pharmaceutically acceptable salts, which comprises: (a) provision of compound of (5RS)-5-(4-methoxyphenyl)-3-methyl-1-oxa-3-azaspiro[5,5]undecane, namely the spiro-venlafaxine; (b) conversion of spiro-venlafaxine into spiro-venlafaxine hydrochloride salt and isolation of said salt in pure form; (c) obtaining O-desmethyl Venlafaxine free base in a one-pot process using spiro-venlafaxine hydrochloride salt as starting material, wherein said one-pot process of step is performed by first O-demethylating of the spiro-venlafaxine hydrochloride obtained from step (b) and subsequently treating the reaction mass with paraformaldehyde, formic acid and water at elevated temperature, preferably from about 105° C. to about 1-10° C., to obtain O-desmethyl Venlafaxine free base.
地址 Pallini Atikis GR