The first synthesis of methyl 2-(4-hydroxy-2-oxo-2H-chromen-3-yl)-2-oxoacetate is described. This compound has been successfully used in a multicomponent enol-Ugi condensation with imines and isocyanides affording 4-aminoacyl-coumarin enamines in a highly atom-economic and convergent process. Furthermore, the postcondensation transformation of these adducts allows the straightforward synthesis of both unprotected amino amides and as yet unknown 2-hydroxychromenyl enamines.

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