Biginelli reaction of β-ketophosphonates, aromatic or aliphatic aldehydes and urea derivatives

Abstract

The synthesis of 3,4-dihydropyrimidin-2(1H)-one phosphonates by the Biginelli reaction of β-ketophosphonates, aldehydes and urea derivatives was studied under microwave conditions. The molar ratio of the starting materials, temperature and reaction time was changed to find the optimal parameters. An efficient zinc-triflate-catalyzed solvent-free method was developed. The condensation was extended and carried out with different β-ketophosphonates, aromatic or aliphatic aldehydes and urea derivatives.

Graphical Abstract

Keywords:

• 3,4-Dihydropyrimidin-2(1H)-one phosphonates
• Biginelli reaction
• multicomponent reaction
• microwave

Additional information

Funding

The project was supported by the Hungarian Research Development and Innovation Office (FK123961). N.P.-T. was supported by the Servier-Beregi PhD Research Fellowship. E.B. was supported by the János Bolyai Research Scholarship of the Hungarian Academy of Sciences (BO/00278/17/7).