Piperidinylpyrroles:: Design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands

被引:45
|
作者
Haubmann, C [1 ]
Hübner, H [1 ]
Gmeiner, P [1 ]
机构
[1] Univ Erlangen Nurnberg, Dept Med Chem, Emil Fischer Ctr, D-91052 Erlangen, Germany
关键词
D O I
10.1016/S0960-894X(99)00540-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Piperidinylpyrroles of type 3 were synthesized through a modified Paal-Knorr reaction. For the introduction of pyrrole-substituents high yielding transformations including Sonogashira cross-coupling reactions were utilized. Employment of the reagent TosMIC gave access to the regioisomeric oxazolyl derivatives 7 and 11 which showed the highest dopamine D4 receptor binding of the series investigated. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3143 / 3146
页数:4
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