期刊
ACS COMBINATORIAL SCIENCE
卷 17, 期 1, 页码 1-4出版社
AMER CHEMICAL SOC
DOI: 10.1021/co5001037
关键词
Suzuki-Miyaura cross-coupling; DNA-encoded library technology
The Suzuki-Miyaura cross-coupling is one of the most widely employed reactions in medicinal chemistry. To apply this reaction to DNA-encoded library technology (ELT), an alternative approach in the discovery of small molecule hits and leads, we explored the Suzuki-Miyaura cross-coupling on DNA-linked aryl halides. Pd(PPh3)4 was demonstrated to be an effective catalyst for cross-coupling with on-DNA halide substrates under aqueous conditions. It efficiently catalyzes the coupling of phenyl halides (iodide or bromide) and pyridinyl bromides with various boronic acids/esters, including challenging heterocyclic boronic acids/esters.
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