56875-96-8

Upstream product

• 1132702-82-9 [(3,4-dimethoxyphenyl)hydroxymethyl]-urea 
• 141-97-9 ethyl acetoacetate 
• 57-13-6 urea 
• 253453-31-5 2-(3,4-dimethoxy)phenyltetrahydro-(2H)-1,3-oxazine 
• 120-14-9 3,4-dimethoxy-benzaldehyde 

Downstream Products

• 893597-09-6 ethyl 1,2-dihydro-4-(3,4-dimethoxyphenyl)-6-methyl-2-oxopyrimidine-5-carboxylate 
• 1445609-60-8 ethyl 6-(dichloromethyl)-4-(3,4-dimethoxyphenyl)-1,2,3,4-tetrahydro-2-oxopyrimidine-5-carboxylate 

Relevant academic research and scientific papers

Deep eutectic solvent mediated synthesis of 3,4-dihydropyrimidin-2(1H)-ones and evaluation of biological activities targeting neurodegenerative disorders

Substitution of hazardous and often harmful organic solvents with “green” and “sustainable” alternative reaction media is always desirous. Ionic liquids (IL) have emerged as valuable and versatile liquids that can replace most organic solvents in a variet

Deep eutectic solvent assisted synthesis of dihydropyrimidinones/thionesviaBiginelli reaction: theoretical investigations on their electronic and global reactivity descriptors

Deep eutectic solvents formed from hydrated metal chlorides and hydrogen bond donors (Type 4) were prepared and their catalytic activity was compared for the synthesis of dihydropyrimidinones/thionesviaBiginelli reaction at room temperature. The one-pot m

Amino acid ionic liquid-catalyzed synthesis, anti-Leishmania activity, molecular docking, molecular dynamic simulation, and ADME study of 3,4-dihydropyrimidin-2(1H)-(thio)ones

The synthesis of 3,4-dihydropyrimidin-2(1H)-(thio)one (DHPM) derivatives involving aromatic aldehyde, β-ketoesters and urea/thiourea using prolinium hydrogen sulfate (ProHSO4) as a catalyst has been studied. A variety of DHPM derivatives were o

A Br?nsted acidic ionic liquid anchored to magnetite nanoparticles as a novel recoverable heterogeneous catalyst for the Biginelli reaction

In this study, simple and effective methods were used for the preparation of an ionic liquid that immobilized magnetite nanoparticles. Fe3O4nanoparticles were preparedviaa chemical co-precipitation method. Then, a SiO2shel

Discovery of new phenyl sulfonyl-pyrimidine carboxylate derivatives as the potential multi-target drugs with effective anti-Alzheimer's action: Design, synthesis, crystal structure and in-vitro biological evaluation

Alzheimer's disease (AD) is multifactorial, progressive neurodegeneration with impaired behavioural and cognitive functions. The multitarget-directed ligand (MTDL) strategies are promising paradigm in drug development, potentially leading to new possible therapy options for complex AD. Herein, a series of novel MTDLs phenylsulfonyl-pyrimidine carboxylate (BS-1 to BS-24) derivatives were designed and synthesized for AD treatment. All the synthesized compounds were validated by 1HNMR, 13CNMR, HRMS, and BS-19 were structurally validated by X-Ray single diffraction analysis. To evaluate the plausible binding affinity of designed compounds, molecular docking study was performed, and the result revealed their significant interaction with active sites of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The synthesized compounds displayed moderate to excellent in vitro enzyme inhibitory activity against AChE and BuChE at nanomolar (nM) concentration. Among 24 compounds (BS-1 to BS-24), the optimal compounds (BS-10 and BS-22) displayed potential inhibition against AChE; IC50 = 47.33 ± 0.02 nM and 51.36 ± 0.04 nM and moderate inhibition against BuChE; IC50 = 159.43 ± 0.72 nM and 153.3 ± 0.74 nM respectively. In the enzyme kinetics study, the compound BS-10 displayed non-competitive inhibition of AChE with Ki = 8 nM. Respective compounds BS-10 and BS-22 inhibited AChE-induced Aβ1-42 aggregation in thioflavin T-assay at 10 μM and 20 μM, but BS-10 at 10 μM and 20 μM concentrations are found more potent than BS-22. In addition, the aggregation properties were determined by the dynamic light scattering (DLS) and was found that BS-10 and BS-22 could significantly inhibit self-induced as well as AChE-induced Aβ1-42 aggregation. The effect of compounds (BS-10 and BS-22) on the viability of MC65 neuroblastoma cells and their capability to cross the blood-brain barrier (BBB) in PAMPA-BBB were further studied. Further, in silico approach was applied to analyze physicochemical and pharmacokinetics properties of the designed compounds via the SwissADME and PreADMET server. Hence, the novel phenylsulfonyl-pyrimidine carboxylate derivatives can act as promising leads in the development of AChE inhibitors and Aβ disaggregator for the treatment of AD.

Natural dolomitic limestone-catalyzed synthesis of benzimidazoles, dihydropyrimidinones, and highly substituted pyridines under ultrasound irradiation

Natural dolomitic limestone (NDL) is employed as a heterogeneous green catalyst for the synthesis of medicinally valuable benzimidazoles, dihydropyrimidinones, and highly functionalized pyridines via C–N, C–C, and C–S bond formations in a mixture of ethan

Synthesis and characterization of the immobilized polythiophene on magnetic carbon nanotube as a prominent catalyst for the synthesis of dihydropyrimidinone and octahydroquinazolinone derivatives

Abstract: In this work, the immobilized polythiophene on magnetic carbon nanotube (CNT–Fe3O4–PTh) was synthesized and introduced as a novel and recoverable catalytic system. The prepared magnetic heterogeneous nanocatalyst was characterized by FT-IR, TGA, EDX, VSM, XRD, TEM, and FE-SEM. Next, the catalytic efficiency of CNT–Fe3O4–PTh was evaluated through the green synthesis of a variety of dihydropyrimidinone and octahydroquinazolinone through Biginelli reaction between aromatic aldehydes, urea/thiourea, and β-dicarbonyl compounds under solvent-free conditions. The catalyst was magnetically recovered and recycled for five cycles without a discernible loss in its catalytic activity. Simple workup, affordability, short reaction times, mild reaction conditions, and the high yield of products are the interesting features of this project. Graphic abstract: An environmentally benign nanocomposite was prepared using carbon nanotube as an inexpensive, nontoxic, and stable support in the preparation of CNT–Fe3O4–PTh, which was efficiently used as catalyst for the green synthesis of dihydropyrimidinone and octahydroquinazolinone derivatives through Biginelli reaction under solvent-free conditions.[Figure not available: see fulltext.].

Synthesis, cytotoxic assessment, and molecular docking studies of 2,6-diaryl-substituted pyridine and 3,4-dihydropyrimidine-2(1H)-one scaffolds

Cancer is one of the main global health problems. In order to develop novel antitumor agents, we synthesized 3,4-dihydropyrimidine-2(1H)-one (DHPM) and 2,6-diaryl-substituted pyridine derivatives as potential antitumor structures and evaluated their cytot

Novel catalytic application of Ni@ZnO nanoparticles and ZnO nanoflakes in aqueous solution of NaPTS hydrotrope at room temperature via a green synthesis of 3,4-dihydropyrimidin-2(1H)-ones

We investigated a novel catalytic application of nickel-doped zinc oxide (Ni-ZnO) nanoparticles and zinc oxide (ZnO) nanoflakes at room temperature in an aqueous hydrotropic solution for the synthesis of biologically active dihydropyrimidones (DHPMs). Ni-

N-Donor ligand activation of titanocene for the Biginelli reaction via the imine mechanism

The remarkable activation of stable titanocene dichloride (Cp2TiCl2) was achieved using N-donor ligand urea in an alcoholic solvent, leading to the formation of a Ti(iv) species [(MeO)2Ti(NHCONH2)]+,