申请人:Shionogi & Co., Ltd.
公开号:EP2687515A1
公开(公告)日:2014-01-22
Disclosed is a process for producing a pyrazole carboxylic acid derivative which is useful as a significant intermediate of an 11βHSD-1 inhibitor.
A compound represented by the Formula (XI):
is useful as a significant intermediate of an 11βHSD-1 inhibitor,
wherein R1 and R2 are each independently hydrogen or substituted or unsubstituted alkyl, R3 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocyclyl and R4 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocyclyl.
本发明公开了一种吡唑羧酸衍生物的生产工艺,该衍生物可用作 11βHSD-1 抑制剂的重要中间体。
由式(XI)代表的化合物:
可用作 11βHSD-1 抑制剂的重要中间体、
其中 R1 和 R2 各自独立地为氢或取代或未取代的烷基,R3 为取代或未取代的烷基、取代或未取代的烯基、取代或未取代的炔基、取代或未取代的环烷基、取代或未取代的环烯基、取代或未取代的芳基、取代或未取代的杂芳基或取代或未取代的杂环基,且 R4 是取代或未取代的烷基、取代或未取代的烯基、取代或未取代的炔基、取代或未取代的环烷基、取代或未取代的环烯基、取代或未取代的芳基、取代或未取代的杂芳基或取代或未取代的杂环基。