VESAMICOL PIPERAZINE DERIVATIVES AND DRUGS CONTAINING THE SAME
申请人:DAIICHI RADIOISOTOPE LABORATORIES, LTD.
公开号:EP1205473A1
公开(公告)日:2002-05-15
A vesamicol piperazine derivative or a salt thereof of the following formula (I) is disclosed.
wherein R is a hydrogen atom, amino group, nitro group, non-radioactive or radioactive iodine atom, trialkyl tin group, or trialkyl silyl group, and A is a substituted or unsubstituted aryl group or a heterocyclic group.
The compound exhibits bonding properties precisely reflecting cholinergic neurons and high affinity to vesamicol receptors, and can specifically diagnose brain diseases, especially, Alzheimer's disease.
本发明公开了一种下式(I)的维沙米醇哌嗪衍生物或其盐。
其中 R 是氢原子、氨基、硝基、非放射性或放射性碘原子、三烷基锡基或三烷基硅基,A 是取代或未取代的芳基或杂环基。
该化合物具有精确反映胆碱能神经元的键合特性以及与维沙米醇受体的高亲和性,可特异性诊断脑部疾病,尤其是阿尔茨海默氏症。
Formation of Arenesvia Diallylarenes: Strategic Utilization of Suzuki–Miyaura Cross-Coupling, Claisen Rearrangement and Ring-Closing Metathesis
作者:Sambasivarao Kotha、Vrajesh R. Shah、Kalyaneswar Mandal
DOI:10.1002/adsc.200600469
日期:2007.5.7
benzoannulation are reported. The first strategy is based on the Suzuki–Miyauracross-coupling reaction. To this end, various ortho-diallylbenzene derivatives were prepared from the corrresponding diiodo derivatives by an allylation strategy using an allylboronate as coupling partner. These diallyl derivatives were subjected to a ring-closingmetathesis (RCM) and one-pot dichlorodicyanoquinone (DDQ) oxidation