申请人:Rikagaku Kenkyusho
公开号:US04324895A1
公开(公告)日:1982-04-13
The present invention relates to a novel process for producing pyrimidine nucleosides by a reaction between bis(tri-lower alkylstannyl)-5-halogenouracil and 2-substituted tetrahydrofurane. The novel process of the present invention makes it possible to obtain, depending upon the manner of substitution of tetrahydrofurane residue on two nitrogen atoms N.sub.1 and N.sub.3 of 5-halogenouracil, N.sub.1 -mono-substituted compound, N.sub.3 -mono-substituted compound and N.sub.1,N-di-substituted compound among which the last can be converted by hydrolysis thereof into N.sub.1 -mono-substituted compound. The present invention further relates to novel N.sub.3 -mono-substituted compounds and N.sub.1,N.sub.3 -di-substituted compounds obtained by such process. The present invention still further relates to novel bis-(tri-lower alkylstannyl)-5-halogenouracil used in the present invention as a raw compound.
本发明涉及一种通过双(三低烷基锡基)-5-卤代尿嘧啶与2-取代四氢呋喃之间的反应来生产嘧啶核苷的新工艺。本发明的新工艺使得根据四氢呋喃残基在5-卤代尿嘧啶的两个氮原子N.sub.1和N.sub.3上的取代方式,可以获得N.sub.1-单取代化合物、N.sub.3-单取代化合物和N.sub.1,N-二取代化合物,其中最后一种可以通过水解转化为N.sub.1-单取代化合物。本发明还涉及通过这种工艺获得的新型N.sub.3-单取代化合物和N.sub.1,N.sub.3-二取代化合物。本发明还涉及作为原料化合物在本发明中使用的新型双(三低烷基锡基)-5-卤代尿嘧啶。