An improved synthesis of Biginelli-type compounds via phase-transfer catalysis

3,4-Dihydropyrimidin-2(1H)-one, 3,4-dihydropyrimidin-2(1H)-thione, and 3,4-dihydropyrimidin-2(1H)-imine derivatives were synthesized by modified Biginelli cyclocondensation reaction in a time-efficient manner with near quantitative yields starting from appropriately substituted aromatic aldehyde, β-ketoester and either urea, thiourea or guanidine as constituent synthons using tetra-butyl ammonium bromide (TBAB) as catalyst for the first time.

3,4-Dihydropyrimidin-2(1H)-one, 3,4-dihydropyrimidin-2(1H)-thione, and 3,4-dihydropyrimidin-2(1H)-imine derivatives were synthesized by modified Biginelli reaction from appropriately substituted aromatic aldehyde, β-ketoester and either urea, thiourea or guanidine using tetra-butyl ammonium bromide (TBAB) as catalyst for the first time in time-efficient manner and in near quantitative yields.