This chapter summarizes multicomponent reactions based on amino acids and their derivatives in the heterocycles chemistry. It provides the classification of multicomponent reactions of amino acids and derivatives according to the ring size of heterocyclic compounds in five categories: Four-membered heterocycles, Five-membered heterocycles, Six-membered heterocycles, Seven-membered heterocycles and fused heterocycles. Chiral β-amino acids constitute interesting building blocks for the synthesis of chiral β-lactams. One of the recent reports on this concept is the synthesis of conformationally constrained tricyclic β-lactam enantiomers through Ugi four-center, three-component reactions of a monoterpene-based β-amino acid. The chapter discusses the synthesis of β-lactam peptidomimetics through Ugi MCR. It describes the stereoselective synthesis of fully substituted tetrahydrofurans through 1, 3-dipolar cycloaddition with cinnamaldehydes. The chapter focuses on the occurrence of an oxidative pathway mediated by highly reactive 2(1H)pyrazinoium salts leads to the first direct preparative method for the straightforward assembly of diversely decorated pyrazin-2,3-(1H,4H)-diones.