Synthesis of p38 MAP kinase inhibitor BIRB 796 and analogs via copper-mediated N-arylation reaction

被引:1
|
作者
Tan, Zhulin [1 ]
Song, Jinhua J. [1 ]
Reeves, Jonathan T. [1 ]
Fandrick, Daniel R. [1 ]
Lee, Heewon [1 ]
Campbell, Scot [1 ]
Yee, Nathan K. [1 ]
机构
[1] Boehringer Ingelheim Pharmaceut Inc, Dept Chem Dev, Ridgefield, CT 06877 USA
关键词
ARYLBORONIC ACID; UREAS; AMINES;
D O I
10.1016/j.tetlet.2010.06.109
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Direct N-arylation of urea (5) with various arylboronic acids mediated by cupric acetate furnished BIR8796 and a range of N-substituted BIRB796 analogs in good to moderate yields in one step. Urea (5) was readily synthesized from commercially available compounds. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4547 / 4551
页数:5
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