Total synthesis of dehydroaltenusin

被引:59
作者
Kamisuki, S
Takahashi, S [1 ]
Mizushina, Y
Hanashima, S
Kuramochi, K
Kobayashi, S
Sakaguchi, K
Nakata, T
Sugawara, F
机构
[1] RIKEN, Inst Phys & Chem Res, Wako, Saitama 3510198, Japan
[2] Sci Univ Tokyo, Dept Appl Biol Sci, Noda, Chiba 2788510, Japan
[3] Kobe Gakuin Univ, Dept Nutrit Sci, Kobe, Hyogo 6512180, Japan
[4] Sci Univ Tokyo, Genome & Drug Discovery Res Ctr, Chiba 2788510, Japan
基金
日本学术振兴会;
关键词
dehydroaltenusin; DNA polymerase alpha; enzyme inhibitor;
D O I
10.1016/j.tet.2004.05.017
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The first total synthesis of dehydroaltenusin, a natural enzyme inhibitor, is described. The key step involves Suzuki-coupling reaction of an aryl triflate prepared from 2,4,6-trihydroxybenzoic acid with a catechol-derived boronic acid or boronic ester. The synthetic product was evaluated as a potent inhibitor against eukaryotic DNA polymerase a and other DNA polymerases. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5695 / 5700
页数:6
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