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The manuscript describes a synthetic route for the formation of 5‐(methylisoindole‐1,3‐dione) pyrimidinones by [4+2] cycloaddition reactions of functionalized 1,3‐diazabuta‐1,3‐dienes with 2‐(3‐Oxo‐allyl)‐isoindole‐1,3‐dione generated in situ from phthaloylalanine and tosyl chloride using triethylamine as a base. The functionalized 5‐(methylisoindole‐1,3‐dione) pyrimidinones were further explored in the deprotection of amines to afford a variety of 5‐methylamino pyrimidinones. The synthesis of such functionalized pyrimidinones is significant as they have a wide range of pharmacological profiles and are valuable as organic synthons. Mechanistic insights are also proposed for the given synthetic methodology. [ABSTRACT FROM AUTHOR]

The functionalization of β-lactams at C-3 position are useful for the strategic improvement in both the dimensions, namely synthetic utility, as versatile intermediate in organic synthesis and biological potential of these heterocyclic systems. The present manuscript involved the π-facial selective synthesis β-lactam hybrids employing highly regioselective and diastereoselective Oxo-Diels-Alder reaction of diethyl ketomalonate with α-dienyl-β-lactam with stereocentres at its α- and β-positions. This protocol provided the cycloaddition of α- and β-stereocentric diene with symmetrical heterodienophiles forming biologically potent regioselective and diastereoselective α-lactams substituted pyrano bifunctional hybrids in good yields and β-facially selectivity. [ABSTRACT FROM AUTHOR]