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多功能三氮烯连接基在杂环文库高效固相合成中的作用

The virtue of the multifunctional triazene linkers in the efficient solid-phase synthesis of heterocycle libraries.

作者信息

Bräse Stefan

机构信息

Institut für Organische Chemie, Universität Karlsruhe (TH), Fritz-Haber-Weg 6, D-76131 Karlsruhe, Germany.

出版信息

Acc Chem Res. 2004 Oct;37(10):805-16. doi: 10.1021/ar0200145.

Abstract

With the implementation of combinatorial chemistry into the modern drug discovery process, the approach to novel diverse heterocycle libraries is an indispensable requirement. Triazenes, which are concealed diazonium salts, can be used to link functionalized arenes and amines to generate various heterocyclic structures, namely, benzoannelated nitrogen heterocycles, upon cleavage from the resin. Since triazene anchors are stable toward various reagents and perform well under a range of reaction conditions, these multifunctional linkers are well suited for automated solid-phase syntheses and the syntheses of complex organic molecules, such as natural products, on solid supports.

摘要

随着组合化学应用于现代药物发现过程,构建新型多样的杂环文库的方法成为一项不可或缺的要求。三氮烯作为潜在的重氮盐,可用于连接官能化芳烃和胺,从树脂上裂解后生成各种杂环结构,即稠合苯环的含氮杂环。由于三氮烯连接基对各种试剂稳定,且在一系列反应条件下表现良好,这些多功能连接基非常适合自动化固相合成以及在固体载体上合成复杂有机分子,如天然产物。

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