A Green, Expeditious, One-Pot Synthesis of 3, 4-Dihydropyrimidin-2(1H)-ones Using a Mixture of Phosphorus Pentoxide-Methanesulfonic Acid at Ambient Temperature

Abstract

An expeditious, one-pot method for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones using a mixture of phosphorus pentoxide-methanesulfonic acid (Eaton's reagent) at room temperature under solvent-free conditions is described. The salient features of this method include short reaction time, green aspects, high yields, and simple procedure.

Eaton’s Reagent Catalyzed Synthesis, Invitro α-Amylase Inhibitory Activity and Molecular Docking Study of some Schiff’s Bases as Diabetic-II Inhibitors

“…Philip Eaton firstly synthesized it in 1973. Eaton's reagent has been used for the synthesis of phenanthrolines, 20 tetrahydroisoquinoline-2ones, 21 quinolones, 22 3,4-dihydropyrimidin-2(1H)-ones, 23 polyamidines 24 and chalcones. 25 Thus, considering the widespread applications, biological significance of Schiff's bases in various fields and in continuation of our successful attempts in the development of bioactive heterocyclic compounds, [26][27] in the present article we report the synthesis of some Schiff's bases from p-tolyl sulphonyl hydrazide and various aldehydes using Eaton's reagent under solvent-free conditions (Scheme 1).…”

A Green Approach for the Synthesis of 2,4-Dihydro-pyrimidinones Using PTSA

“…Several methods improved the procedure using phosphorus pentoxide-methanesulfonic acid 4 , potassium ter-butoxide (t-BuOK) 5 , ammonium dihydrogen phosphate 6 , silica-gel 7 , mesoporous molecular sieve MCM-41 8 , cyanuric chloride 9,10 , nano-BF 3 ⋅SiO 2 silica gel supported polyphosphoric acid 11 , zirconium(IV) chloride 12 , and indium(III) bromide 13 14 have been employed for this transformation.…”

Untitled

“…5 In further years, improvement in Biginelli compounds is done by using different catalysts such as polyphosphate ester (PPE) 6 , Bronsted acids viz. p-toluenesulfonic acid 7 , potassium hydrogen sulphate 8 , chloroacetic acid 9 , titanium (IV) chloride 10 , ruthenium (III) chloride 11 , scandium (III)triflate 12 , Iodine-alumina 13 ,Cobalt(II)acetate 14 ,sulphated zirconia 15 , ferric chloride hexahydrate 16 , MgBr 2 17 , nbcl 5 18 , Lewis acids 19,20 viz. Yb (OTf) 3 21 , InCl 3 22 , CuCl 2 23 , SnCl 2 24 , BF 3 .OEt 2 25 , ZrCl 4 26 , L-proline 19 , L-proline methylester hydrochloride 27 , ZnCl 2 28, 29 , Zinc sulphamate 30 , combination catalytic system such as tin chloridelithium chloride 31 , cupric chloride-lithium chloride 32 , ferric chloride/tetraethyl orthosilicates 33 , Trimethylsilyl triflate 34 , strontium(II)triflate 35 , cadmium chloride 36 , methanesulfonic acid 37 , Iron(III) 38 , (AlCl 3 +KI) 39 , bimetal system , Cupy 2 Cl 2 40 , Samariumdiiodide 41 .…”