公开(公告)号：EP3015455A1

公开(公告)日：2016-05-04

申请号：EP14817699.3

申请日：2014-06-23

申请人： Zhejiang Hisun Pharmaceutical Co. Ltd. ,  Shanghai Institute Of Pharmaceutical Industry

发明人： ZHANG, Fuli ,  YANG, Zhezhou ,  BAO, Rusheng ,  QIU, Pengcheng ,  JIN, Linyong ,  PAN, Hu ,  PAN, Linyu ,  JIANG, Dongming ,  XU, Weiwei

IPC分类号： C07C237/06 ,  C07C231/02 ,  C07D241/08 ,  C07D471/04

CPC分类号： C07C237/06 ,  C07C231/02 ,  C07C231/10 ,  C07D241/08 ,  C07D471/04

摘要： The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.

摘要翻译： 本发明提供的一个关键新的中间4-苄基-1-苯乙基 - 哌嗪-2,6-二酮（式IV化合物），其药学上可接受的盐和它们的制备方法（式III的化合物）。 此外，本发明盘松的方法用于从式III化合物制备4-苄基-1-苯乙基 - 哌嗪-2,6-二酮（式IV化合物），所述方法克服了当前的式IV化合物的制备方法的短缺憾，：如 低生产量，低纯度，高能耗，成本高，而且无法实现工业化生产，并提供了式IV化合物的制备方法，其全部是简单，经济，环境友好且易于生产工业上; 该方法的反应溶剂容易回收，并且该方法可产生在高生产率和高纯度的式IV化合物。