申请人:Kasai Kiyoshi
公开号:US20090062518A1
公开(公告)日:2009-03-05
The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like.
A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula:
wherein R
1
, R
2
, R
3
, R
4
and R
5
may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R
6
is an alkyl group, for example R
7
is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula:
wherein as an example, PG
1
is a pivaloyl group or the like, as an example, X
1
is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.
本发明涉及一种制备葡萄糖吡唑氧基吡唑衍生物的方法,该衍生物可用作预防或治疗与高血糖相关的疾病,如糖尿病、糖尿病并发症、肥胖症等的药物。通过让一个苄基吡唑衍生物与一个化合物反应,可以轻松高效地制备葡萄糖吡唑氧基吡唑衍生物。其中,该苄基吡唑衍生物由下列通式表示:其中R1、R2、R3、R4和R5可以相同也可以不同,例如每个都是氢原子、卤素原子或烷基、烷氧基、芳基甲氧基等,R6是烷基,例如R7是氢原子或烷基、烷氧基、芳基甲氧基等。化合物由下列通式表示:其中,PG1是一个Pivaloyl基团或类似物,例如,X1是溴原子或类似物。因此,本发明作为一种制备药物化合物的方法非常有用。