Application of Suzuki-Miyaura and Buchwald-Hartwig Cross-coupling Reactions to the Preparation of Substituted 1,2,4-Benzotriazine 1-Oxides Related to the Antitumor Agent Tirapazamine.
Application of Suzuki-Miyaura and Buchwald-Hartwig Cross-coupling Reactions to the Preparation of Substituted 1,2,4-Benzotriazine 1-Oxides Related to the Antitumor Agent Tirapazamine.
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DOI：
10.1002/jhet.2559
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发表时间：
2017-01
影响因子：
2.4
通讯作者：
Gates KS
中科院分区：
文献类型：
--
作者：
Sarkar U;Hillebrand R;Johnson KM;Cummings AH;Phung NL;Rajapakse A;Zhou H;Willis JR;Barnes CL;Gates KS
许多 1,2,4-苯并三嗪 1,4-二氧化物表现出选择性杀死实体瘤中发现的缺氧细胞的能力。因此，需要能够获得取代的1,2,4-苯并三嗪1-氧化物的合成路线，其可用作合成1,2,4-苯并三嗪1,4-二氧化物的直接前体。在这里，我们描述了使用 Suzuki-Miyaura 和 Buchwald-Hartwig 交叉偶联反应来构建在 3-、6-和 7-位上带有取代基的各种 1,2,4-苯并三嗪 1-氧化物类似物。
Many 1,2,4-benzotriazine 1,4-dioxides display the ability to selectively kill the oxygen-poor cells found in solid tumors. As a result, there is a desire for synthetic routes that afford access to substituted 1,2,4-benzotriazine 1-oxides that can be used as direct precursors in the synthesis of 1,2,4-benzotriazine 1,4-dioxides. Here we describe the use of Suzuki-Miyaura and Buchwald-Hartwig cross-coupling reactions for the construction of various 1,2,4-benzotriazine 1-oxide analogs bearing substituents at the 3-, 6-, and 7-positions.