Synthesis of Nτ-arylhistidine derivatives via direct N-arylation

被引:12
|
作者
Yue, WM [1 ]
Lewis, SI [1 ]
Koen, YM [1 ]
Hanzlik, RP [1 ]
机构
[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA
关键词
N-arylation; aryl halides; histidine derivatives; Ullmann type coupling;
D O I
10.1016/j.bmcl.2004.01.058
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
N-tau-Aryl-histidine derivatives were synthesized using a modified one-step Cu-catalyzed coupling of aryl halides and N-acetylhistidine methyl ester. The latter is much less reactive than imidazole toward aryl halides. p-Chloroiodobenzene coupled with iodine displacement only, whereas m- and p-bromoiodobenzene both gave mixtures of bromo- and iodophenyl products. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1637 / 1640
页数:4
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