TsCl/DBU-Mediated CO2 Carbonylation for 1,3-Disubstituted Imidazolidin-2-ones and Tetrahydropyrimidin-2(1H)-ones Under Mild Conditions.

A novel TsCl/DBU-mediated CO2 carbonylation protocol has been developed for the efficient synthesis of disubstituted imidazolidin-2-one and tetrahydropyrimidin-2-one derivatives from N1-arylmethyl-N2-arylethane-1,2-diamines or N1-arylmethyl-N3-arylpropane-1,3-diamines. The reaction proceeds under mild conditions at atmospheric pressure without requiring any metal catalyst. Notably, this protocol avoids high temperature, high pressure, and transition-metal catalysts. The method features a broad substrate scope, excellent functional group tolerance, short reaction times, and operational practicality, offering a useful strategy for accessing functionalized carbonyl-containing heterocycles. Preliminary biological evaluation reveals that several synthesized compounds exhibit promising antifungal activity.