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Efficient Biginelli Synthesis of 2-Aminodihydropyrimidines under Microwave Irradiation

Fulvia Felluga*, Fabio Benedetti, Federico Berti, Sara Drioli, Giorgia Regini

*Dipartimento di Scienze Chimiche e Farmaceutiche, UniversitÓ di Trieste, via L. Giorgieri 1, I-34127 Trieste, Italy, Email:

F. Felluga, F. Benedetti, F. Berti, S. Drioli, G. Regini, Synlett, 2018, 29, 986-992.

DOI: 10.1055/s-0036-1591900 (free Supporting Information)

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A practical and general microwave-mediated Biginelli cyclocondensation of guanidine with aldehydes and β-dicarbonyl compounds provides functionalized 2-amino-3,4-dihydropyrimidines in good yields, with short reaction times and a simple workup. The scope is considerably wider than that of similar reactions carried out under conventional heating.

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Key Words

Biginelli reaction, microwave synthesis, guanidine, dicarbonyl compounds, aminodihydropyrimidines, multicomponent reactions

ID: J60-Y2018