公开(公告)号：EP3070094A1

公开(公告)日：2016-09-21

申请号：EP14861246.8

申请日：2014-04-28

申请人： Zhejiang Hisun Pharmaceutical Co. Ltd.

发明人： GUO, Yanghui ,  ZHOU, Junhui ,  CAI, Qingfeng ,  WEI, Hegeng ,  BAI, Hua ,  LONG, Fei ,  ZHANG, Yue ,  WU, Yingqiu

IPC分类号： C07H13/08 ,  C07H3/10 ,  C07H1/00

CPC分类号： C07H11/00 ,  C07H1/00 ,  C07H3/10 ,  C07H13/04 ,  C07H13/08 ,  C07H17/04

摘要： The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.

摘要翻译： 本发明涉及二糖中间体及其合成方法，涉及化学药物领域，更具体地涉及一种用于化学合成肝素和类肝素化合物的关键中间体的二糖片段的制备方法。 公开了一种新的二糖中间体和三种合成二糖中间体的方法，即式（4）化合物和被不同异头碳保护的吡喃葡萄糖在活性剂存在下反应，得到二糖中间体。 根据本发明的技术方案，合成原料容易获得，反应条件温和，适合工业化生产。