发明授权
EP2229351B1 PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE
有权
生产高纯度2- [4-(3-或2-氟苯氧基)苄基氨基]丙酰胺的方法
- 专利标题: PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE
- 专利标题(中): 生产高纯度2- [4-(3-或2-氟苯氧基)苄基氨基]丙酰胺的方法
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申请号: EP08860373.3申请日: 2008-12-01
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公开(公告)号: EP2229351B1公开(公告)日: 2017-11-08
- 发明人: BARBANTI, Elena , FARAVELLI, Laura , SALVATI, PATRICIA , CANEVOTTI, Renato , PONZINI, Francesco
- 申请人: Newron Pharmaceuticals S.p.A.
- 申请人地址: Via Ariosto, 21 20091 Bresso (MI) IT
- 专利权人: Newron Pharmaceuticals S.p.A.
- 当前专利权人: Newron Pharmaceuticals S.p.A.
- 当前专利权人地址: Via Ariosto, 21 20091 Bresso (MI) IT
- 代理机构: Bianchetti Bracco Minoja S.r.l.
- 优先权: EP07023937 20071211
- 国际公布: WO2009074478 20090618
- 主分类号: C07C231/12
- IPC分类号: C07C231/12 ; C07C251/24 ; C07C237/08 ; A61K31/165 ; A61P25/00
摘要:
A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C 1 -C 5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
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