申请人:SCOTIA HOLDINGS PLC
公开号:EP0317207A2
公开(公告)日:1989-05-24
A process for the production of a 5-substituted derivative of a 2,3′-anhydro-2′-deoxyuridine preferably corresponding to the following general formula:
wherein
R¹ represents H, alkyl, aryl, halogeno or CF₃;
characterised in that it comprises heating a 5-substituted derivative of a 2′-deoxyuridine preferably corresponding to the following general formula:
wherein R¹ is as defined above;
in the presence of a sulphite transfer reagent and preferably a solvent is disclosed.
This process improves the production of valuable intermediates and hence facilitates and reduces the cost of production of pharmacologically-interesting compounds.
一种生产2,3′-脱水-2′-脱氧尿苷的5-取代衍生物的工艺,最好与下式通式相对应:
其中
R¹ 代表 H、烷基、芳基、卤素或 CF₃;
其特征在于,它包括加热 2′-脱氧尿苷的 5-取代衍生物,该衍生物最好与下 列通式相对应:
其中 R¹ 如上定义;
在亚硫酸盐转移试剂和优选溶剂存在下进行。
该工艺提高了有价值中间体的产量,从而促进并降低了有药理作用化合物的生产成本。