DNA結合型アミンからのβ-ケトアミドのDNA適合性合成、およびDNA結合型化学多様化中間体
Xianfeng Li1,2, Zehao Yin2, Qiuyi Chen2
1Pharmaceutical Department, Chongqing University Three Gorges Hospital, Chongqing University, Chongqing 404100, China.
Abstract:
The β-ketoamide motif represents both a privileged scaffold and a versatile synthetic intermediate in medicinal chemistry. Herein, we developed a DNA-compatible method for the efficient conversion of various DNA-conjugated amines into β-ketoamides. The resulting β-ketoamides facilitate rapid diversification into a panel of structurally diverse molecular scaffolds. Importantly, the synthetic route and subsequent derivatization steps were validated to be fully compatible with DNA encoding, offering a reliable and versatile platform for DNA-encoded library synthesis.
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