An efficient and practical method has been developed for the diversity-oriented synthesis of chromone-containing tripeptides via pseudo-five-component reaction between 3-formylchromones, Meldrum's acid, isocyanides and primary aromatic amines for the generation of a wide range of structurally interesting and pharmacologically significant compounds at ambient temperature. It is worth mentioning that in the course of this reaction, five new bonds (two C-C bonds, two C-N bonds and one C═O bond) are formed. In the present reaction three amide bonds are newly formed.
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