An efficient enantioselective classic three-component Passerini reaction with a broad substrate scope in the presence of a chiral phosphoric acid catalyst has been developed. This represents the general example for classic three-component Passerini reaction with good to excellent enantioselectivies involving aromatic aldehydes and the bulky pivalaldehyde under mild reaction conditions. The feature of this method is highlighted by using a chiral phosphoric acid to activate carboxylic acid, aldehyde, and isocyanide for the facile construction of widely useful complex compounds.
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