On-DNA Pd and Cu promoted C-N cross-coupling reactions.

作者:Lu, Xiaojie*; Roberts, Sarah E*; Franklin, George J*; Davie, Christopher P*
来源:MedChemComm, 2017, 8(8): 1614-1617.
DOI:10.1039/c7md00289k

摘要

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.

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