One-Pot Synthesis of α‑Ketoamides from α‑Keto Acids and Amines Using Ynamides as Coupling Reagents

A one-pot strategy for α-keto amide bond formation have been developed by using ynamides as coupling reagents under extremely mild reaction conditions. Diversely structural α-ketoamides were afforded in up to 98% yield for 36 examples. This reaction features advantages such as practical coupling pro...

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Published inJournal of organic chemistry Vol. 87; no. 5; pp. 3661 - 3667
Main Authors Ma, Jianting, Cui, Xue, Xu, Junyu, Tan, Yinfeng, Wang, Yan, Wang, Xuesong, Li, Youbin
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 04.03.2022
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Summary:A one-pot strategy for α-keto amide bond formation have been developed by using ynamides as coupling reagents under extremely mild reaction conditions. Diversely structural α-ketoamides were afforded in up to 98% yield for 36 examples. This reaction features advantages such as practical coupling procedure, wide functional group tolerance, and extremely mild conditions and has potential applications in synthetic and medicinal chemistry.
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ISSN:0022-3263
1520-6904
DOI:10.1021/acs.joc.1c02453