2-aryl indole NK1 receptor antagonists:: Optimisation of the 2-aryl ring and the indole nitrogen substituent

2-aryl indole NK1 receptor antagonists:: Optimisation of the 2-aryl ring and the indole nitrogen substituent
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DOI:
10.1016/s0960-894x(01)00183-4
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发表时间:
2001-05-07
影响因子:
2.7
通讯作者:
Swain, CJ
Swain, CJ
中科院分区:
医学4区
文献类型:
--
作者:
Dinnell, K;Chicchi, GG;Swain, CJ

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合成了新型的2-芳基吲哚HNK(1)受体配体,以钯为中间体的交叉偶联反应为关键步骤。合成了具有较高的HNK(1)受体亲和力和良好的脑渗透性(如9d)的化合物。(C)2001爱思唯尔科学有限公司。保留所有权利。
Novel 2-aryl indole hNK(1) receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK(1) receptor binding affinity and good brain penetration (e.g., 9d) were synthesised. (C) 2001 Elsevier Science Ltd. All rights reserved.