期刊
TETRAHEDRON LETTERS
卷 46, 期 16, 页码 2919-2922出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2005.02.128
关键词
mesylation; pyridinones; dihydropyridobenzothiazepin-lones; anti-HIV; reverse transcriptase
Reaction of 4-hydroxy-3-nitropyridinone 8 with TsCl and MsCl, respectively, resulted in rapid and quantitative formation of ditosylate 13 and dimesylate 16. Through chemoselective reaction of 16 with thiophenol 17 the key 4-thioaryl substituted intermediate 18 was obtained in 78% yield. This compound was efficiently converted to the target tricyclic products 4a and b. Compound 4a, in particular, is a potent inhibitor in vitro (IC50 = 2 nM) of wild type HIV-1 replication. (c) 2005 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据