Synthesis of SMP-797: a new potent ACAT inhibitor

被引:14
作者
Ban, H [1 ]
Muraoka, M [1 ]
Ohashi, N [1 ]
机构
[1] Sumitomo Pharmaceut Co Ltd, Div Res, Kohohana Ku, Osaka 5540022, Japan
关键词
cyclization; Friedlander reaction; Suzuki coupling; 4-selective nitration; SMP-797;
D O I
10.1016/j.tet.2005.08.009
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A potent ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor SMP-797 was effectively synthesized by the urea formation of 3-amino-4-aryl-1,8-naphthyridin-2(1H)-one and 4-amino-2,6-diisopropylamine. The synthesis of the former compound involved the Suzuki coupling reaction as a key step, and the latter was prepared by the 4-selective nitration of 2,6-diisopropylaniline using 2,3,5,6-tetrabromo-4-methyl-4-nitro-2,5-cyclohexadienone. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:10081 / 10092
页数:12
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