The invention provides an improvement in the production of imidazole derivatives including histamine H3 agonist immepip and histamine H3 antagonist VUF4929. Desired imidazole derivatives can be easily obtained in high yield by using novel intermediates represented by the general formula (I):
wherein R1 is an amino-protecting group; R2 and R3 are each independently hydrogen, lower alkyl, or hydroxy-(lower alkyl); R4 is lower alkyl, halogenated lower alkyl, or substituted or unsubstituted phenyl; and A is C1-3 alkylene.
本发明改进了
组胺 H3 激动剂 immepip 和
组胺 H3 拮抗剂 VUF4929 等
咪唑衍
生物的生产工艺。利用通式 (I) 所代表的新型中间体,可以很容易地以高产率获得所需的
咪唑衍
生物:
其中 R1 是
氨基保护基团;R2 和 R3 各自独立地是氢、低级烷基或羟基-(低级烷基);R4 是低级烷基、卤代低级烷基或取代或未取代的苯基;A 是 C1-3 亚烷基。