A simple effective synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives from aromatic aldehydes, 1,3-dicarbonyl compounds and urea in glacical acetic acid using cadmium sulfate as catalyst is described and compared with the classical Biginelli reaction conditions, this new method has the advantage of excellent yields (83–94%) and short reaction time (2-4 h).
AtwalK.S., SwansonB. N., UngerS. E., FloydD. M., MorelandS., HedbergA., and O'ReillyB. C., J. Med. Chem., 1991, 34, 806. G.C. Rovnyak, K.S. Atwal, A. Hedberg, S.D. Kimball, S. Moreland, J.Z. Gougoutas, B.C. O'Reilly, J. Schwart and M.F. Malley, J. Med. Chem., 1992, 35, 3254. G.J. Grover, S. Dzwonczyk, D.M. Mcmullen, C.S. Normadinam, P.G. Slenph and S.J. Moreland, J. Cardiovase. Pharmacol., 1995, 26, 289.
3.
SniderB.B., and ShiZ. P., J. Org. Chem., 1993, 58, 3828. and references therein.
4.
O'ReillyB.C., and AtwalK. S., Heterocycles, 1987, 26, 1185.
