Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand
摘要:
The first selective dopamine D-4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. The specific activity of these two radioligands was measured and [H-3]6b found to be suitable for use in D-4 saturation and competition binding studies. The synthesis, biological, and radioactivity of this new agonist radioligand as well as preliminary SAR will be discussed. (C) 2004 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2004.07.068
作为产物:
描述:
溴乙酰氯 、 3-甲基-2,4,6-三溴苯胺 以
甲苯 为溶剂,
反应 24.0h,
以to provide 2.88 g (49%) of the title compound as a white solid的产率得到2-bromo-N-(2,4,6-tribromo-3-methylphenyl)acetamide
参考文献:
名称:
Acetamides and benzamides that are useful in treating sexual dysfunction
ACETAMIDES AND BENZAMIDES THAT ARE USEFUL IN TREATING SEXUAL DYSFUNCTION
申请人:Abbott Laboratories
公开号:EP1509213A2
公开(公告)日:2005-03-02
US7528134B2
申请人:——
公开号:US7528134B2
公开(公告)日:2009-05-05
[EN] ACETAMIDES AND BENZAMIDES THAT ARE USEFUL IN TREATING SEXUAL DYSFUNCTION<br/>[FR] ACETAMIDES ET BENZAMIDES UTILISES DANS LE TRAITEMENT D'UNE DYSFONCTION SEXUELLE
申请人:ABBOTT LAB
公开号:WO2003099266A2
公开(公告)日:2003-12-04
The present invention relates to the use of compounds of formula (I), for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.