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    PROCESS FOR THE PRODUCTION OF 2-Ý4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO¨PROPANAMIDES WITH HIGH PURITY DEGREE
    1.
    发明公开
    PROCESS FOR THE PRODUCTION OF 2-Ý4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO¨PROPANAMIDES WITH HIGH PURITY DEGREE 有权
    PROCESS FOR制备2- [4-（3-或2-氟苄氧基）苄基氨基] PROPANAMIDEN高纯度

    公开(公告)号：EP2229351A1

    公开(公告)日：2010-09-22

    申请号：EP08860373.3

    申请日：2008-12-01

    申请人： Newron Pharmaceuticals S.p.A.

    发明人： BARBANTI, Elena ,  FARAVELLI, Laura ,  SALVATI, PATRICIA ,  CANEVOTTI, Renato ,  PONZINI, Francesco

    IPC分类号： C07C231/12 ,  C07C251/24 ,  C07C237/08 ,  A61K31/165 ,  A61P25/00

    CPC分类号： C07C251/24 ,  A61K31/165 ,  A61K31/197 ,  A61K31/198 ,  A61K45/06 ,  C07C231/12 ,  C07C231/24 ,  C07C237/08

    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.

    摘要翻译： 一种用于与具有高纯度，即，与二苄基衍生物杂质的含量低于0.03％，以获得治疗活性2- [4-（3-和2-（氟苄氧基）苄基氨基] -propanamides和与药学上可接受的酸及其盐的过程 （重量）。该方法通过提交船基中间体与还原剂的还原反应在有机溶剂中的量，以允许悬浮液的船舶上的（还原反应的相当大的部分中和存在下）形成开展 基地。

    PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE
    4.
    发明公开
    PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE 审中-公开
    生产高纯度2- [4-（3-或2-氟苯氧基）苄基氨基]丙酰胺的方法

    公开(公告)号：EP3257842A1

    公开(公告)日：2017-12-20

    申请号：EP17181175.5

    申请日：2008-12-01

    申请人： Newron Pharmaceuticals S.p.A.

    发明人： BARBANTI, Elena ,  FARAVELLI, Laura ,  SALVATI, Patricia ,  CANEVOTTI, Renato ,  PONZINI, Francesco

    IPC分类号： C07C251/24 ,  A61K31/165 ,  A61P25/00 ,  A61K31/197 ,  A61K31/198 ,  A61K45/06

    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.

    摘要翻译： 一种获得具有高纯度的治疗活性的2- [4-（3-和2-（氟苄氧基）苄基氨基]丙酰胺及其与可药用酸形成的盐的方法，特别是二苄基衍生物杂质含量低于0.03％ 通过使席夫碱中间体2- [4-（3-和2-氟苄氧基）亚苄基氨基]丙酰胺与选自硼氢化钠和钾的还原剂进行还原反应来进行该方法 硼氢化物在合适量的选自C 1 -C 5低级链烷醇的有机溶剂中反应，允许在希夫碱在希夫碱的饱和溶液的悬浮液的还原反应过程的实质位置形成和存在于相同的有机 溶剂。