Abstract
N-Substituted α-amino acid amides can be easily obtained in two steps using the four-component Ugi reaction followed by chemoselective cleavage of the resulting tertiary amide. The use of the sacrificial acid, 2-hydroxymethylbenzoic acid is associated to shorter reaction times, higher yields, and safer and greener reaction conditions compared to strategies based on trifluoroacetic acid, a toxic and environmental hazardous reagent. The optimized procedure was easily scaled up to gram amounts.
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