A New Biginelli Reaction Procedure Using Potassium Hydrogen Sulfate as the Promoter for an Efficient Synthesis of 3,4-Dihydropyrimidin-2(1H)-one

Abstract

Simple and improved conditions have been found to carry out the Biginelli reaction for the synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives. This synthesis was performed using potassium hydrogen sulfate as the promoter in glycol solution. Compared with the classical Biginelli reaction conditions, this new method has the advantage of excellent yields (85-99%) and short reaction time (0.5-2 h).

Three Component Reaction: An Efficient Synthesis of 3,4‐Dihydropyrimidin‐2(1H)‐ones and Thiones Using Heterogeneous Catalyst

“…For the synthesis of dihydropyrimidinones attention has been mainly paid to using open-chained 1,3-dicarbonyl compounds, while the use of cyclic 1,3-dicarbonyl compounds has been seldom reported. 26,28 Therefore, the development of a milder, faster, eco-friendly and high-yielding protocol using cyclic 1,3-dicarbonyl compounds is still of great importance.…”

Magnesium Chloride Hexahydrate Catalyzed One‐Pot Synthesis of 3,4‐Dihydropyrimidin‐2‐(1H)ones Under Solvent‐Free Conditions

“…6H 2 O, [9] p-TsOH, [10] LaCl 3 . 7H 2 O, [11] Bi(OTf) 3 , [12] KHSO 4 , [13] ionic liquids (BMImPF 6 and BMImBF 4 ), [14] Mn(OAc) 3 . 2H 2 O, [15] or TMSOTf [16] as the catalyst.…”

Solvent‐free synthesis of monastrol derivatives catalyzed by NaHSO4

“…However, this oxygenbridged pyrimidine structures were not discussed in several recent reports [13][14][15]20,21], but were supported by others [12,16,17]. The product from reactions involving 5-chloro or 5-bromosalicylaldehyde, methyl (or ethyl) acetoacetate with thiourea is also an oxygen-bridged compounds 5d-g rather than the corresponding 4-(2-hydroxyphenyl)pyrimidines.…”