Abstract

A catalyst‐ and additive‐free chemoselective transfer hydrogenation of α‐keto amides to α‐hydroxy amides is easily achieved by using sodium formate as a hydrogen source. The utility of this method is demonstrated by gram‐scale synthesis and transformation of the resultant α‐hydroxy amides into polysubstituted acetamides and 2‐arylindole derivatives. Control experiments suggest that the NH group of α‐keto amides is crucial for the chemoselective reduction through the formation of hydrogen bonds.

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