Total synthesis of dehydroaltenusin

Total synthesis of dehydroaltenusin
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DOI:
10.1016/j.tet.2004.05.017
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发表时间:
2004-06-28
期刊:
影响因子:
2.1
通讯作者:
Sugawara, F
Sugawara, F
中科院分区:
化学3区
文献类型:
--
作者:
Kamisuki, S;Takahashi, S;Sugawara, F

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报道了天然酶抑制剂脱氢Altenusin的首次全合成。关键步骤涉及由2,4,6-三羟基苯甲酸与邻苯二酚衍生的硼酸或硼酸酯制备的三氟甲磺酸芳基酯的Suzuki偶联反应。合成产物被评价为对真核DNA聚合酶a和其它DNA聚合酶的有效抑制剂。(C)2004 Elsevier Ltd.保留所有权利。
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.