On-DNA Pd and Cu promoted C–N cross-coupling reactions,RSC Medicinal Chemistry

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On-DNA Pd and Cu promoted C–N cross-coupling reactions
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-07-12 00:00:00 , DOI: 10.1039/c7md00289k
Xiaojie Lu _{1,

2,

3,

4,

5} , Sarah E. Roberts _{1,

2,

3,

4,

5} , George J. Franklin _{1,

2,

3,

4,

5} , Christopher P. Davie _{1,

2,

3,

4,

5}

Affiliation

Encoded library technology (ELT) is a novel hit identification platform synergistic with HTS, fragment hit ID and focused screening. It provides both an ultra high-throughput and a cost-efficient tool for the discovery of small molecules that bind to protein targets of pharmaceutical interest. The success of ELT relies heavily on the chemical diversity accessed through DNA-encoded library (DEL) synthesis. We developed unprecedented Pd and Cu(I) promoted C–N cross-coupling reactions between a DNA-conjugated aryl iodide and primary amines. These reported reactions have strong potential for application in DNA-encoded library (DEL) synthesis.

中文翻译：

DNA上的Pd和Cu促进C–N交叉偶联反应

编码库技术（ELT）是与HTS，片段命中ID和集中筛选协同工作的新型命中识别平台。它提供了超高通量和具有成本效益的工具，用于发现与药物目标蛋白质靶标结合的小分子。ELT的成功在很大程度上取决于通过DNA编码文库（DEL）合成获得的化学多样性。我们开发了前所未有的Pd，而Cu（I）促进了DNA共轭芳基碘化物和伯胺之间的C–N交叉偶联反应。这些报道的反应具有很强的应用在DNA编码文库（DEL）合成中的潜力。

更新日期：2017-08-16

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