The introduction of a 1,3‐dicarbonyl unit in curcuminoid derivatives for multi‐component reactions (MCRs) to furnish six‐membered heterocyclic compounds has been reviewed. Attention has focused on the assembly of the three‐component Biginelli reactions relating to curcumin or tetrahydrocurcumin (THC), aromatic aldehydes and urea as substrates. The hybrid molecules of two bioactive agents were designed and synthesized by using these MCRs concepts. The four‐component modified Hantzsch condensation was the latest development of this synthetic route. The possible mechanism of the MCRs of both curcumin and THC were also summarized.

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The title compounds are prepared by Hantzsch reaction of tetrahydrocurcumin, benzaldehydes, and ammonium acetate in moderate yields.