申请人:Sakamoto Yasuhiko
公开号:US20050043277A1
公开(公告)日:2005-02-24
An improvement in the production of imidazole derivatives including histamine H
3
agonist immepip and histamine H
3
antagonist VUF4929. Desired imidazole derivatives can be easily obtained in high yield by using novel intermediates represented by the general formula (I): (I) wherein R
1
is an amino-protecting group; R
2
and R
3
are each independently hydrogen, lower alkyl, or hydroxylated lower alkyl; R
4
is lower alkyl, halogenated lower alkyl, or substituted or unsubstituted phenyl; and A is C
1-3
alkylene.
生产咪唑衍生物,包括组胺H3激动剂immepip和组胺H3拮抗剂VUF4929的方法得到了改进。使用由通式(I)表示的新型中间体,可以轻松地高产得到所需的咪唑衍生物:(I)其中,R1是氨基保护基;R2和R3各自独立地是氢、低碳基或羟基化的低碳基;R4是低碳基、卤代低碳基或取代或未取代的苯基;A是C1-3烷基。