84857-16-9

Upstream product

• 593-85-1 diguanidine carbonate 
• 104-87-0 4-methyl-benzaldehyde 
• 99-91-2 para-chloroacetophenone 
• 19672-63-0 1-(4-chlorophenyl)-3-(4-methylphenyl)prop-2-en-1-one 
• 113-00-8 guanidine nitrate 
• 104-88-1 4-chlorobenzaldehyde 
• 122-00-9 para-methylacetophenone 
• 13565-39-4 3-(4-chlorophenyl)-1-p-tolylprop-2-en-1-one 
• 506-93-4 guanidine nitrate 
• 50-01-1 guanidine hydrochloride 

Downstream Products

• 1229405-56-4 C₁₈H₁₅ClN₄O 
• 1370031-05-2 1-benzylidene-3-[4-(4-chloro-phenyl)-6-p-tolyl-pyrimidin-2-yl]-urea 
• 1229404-98-1 4-[4-(4-chlorophenyl)-6-p-tolylpyrimidin-2-yl]semicarbazide 
• 1370031-06-3 1-[4-(4-chlorophenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(4-chlorobenzylidene)-urea 
• 1370031-07-4 1-[4-(4-chlorophenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(4-nitrobenzylidene)-urea 
• 1370031-08-5 1-[4-(4-chlorophenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(4-methylbenzylidene)-urea 
• 1370031-09-6 1-[4-(4-chloro-phenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(4-dimethylaminobenzylidene)-urea 
• 1370031-10-9 1-[4-(4-chlorophenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(1-p-tolylethylidene)-urea 
• 1370031-11-0 1-[4-(4-chloro-phenyl)-6-p-tolyl-pyrimidin-2-yl]-3-[1-(4-hydroxyphenyl)-ethylidene]-urea 
• 1370031-12-1 1-[4-(4-chloro-phenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(3-chlorobenzylidene)-urea 
• 1370031-13-2 1-[4-(4-chloro-phenyl)-6-p-tolyl-pyrimidin-2-yl]-3-(3-nitrobenzylidene)-urea 
• 1370031-04-1 phenyl 4-(4-chlorophenyl)-6-p-tolylpyrimidin-2-ylcarbamate 
• 1608467-90-8 N-[4-(4-chlorophenyl)-6-(4-methylphenyl)pyrimidin-2-yl]-4-methylbenzenesulfonamide 
• 1608467-85-1 N-[4-(4-chlorophenyl)-6-(4-methylphenyl)pyrimidin-2-yl]benzenesulfonamide 

Relevant academic research and scientific papers

Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors

Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this

Design, synthesis and evaluation of 2,4,6-substituted pyrimidine derivatives as BACE-1 inhibitor: Plausible lead for alzheimer’s disease

Alzheimer’s disease is one of the most common neurodegenerative disorder afflicting a large mass of population. BACE-1 (β-secretase) is an aspartyl protease of the amyloidogenic pathway considered responsible for Alzheimer’s disease (AD). Since it catalyzes the rate-limiting step of Aβ-42 production from amyloid precursor protein (APP), its inhibition is considered a viable thera-peutic strategy. We have reported the design of small molecular weight compounds supposed to be blood brain permeable as BACE-1 inhibitors. The clue for the design of this series is drawn from the previously designed series from our research group. Objective: Design and synthesis of 2,4,6-substituted pyrimidine derivatives has been reported. In vitro FRET-based screening of synthesized derivatives was performed to evaluate the BACE-1 inhibition profile. Methods: Based on the docking simulation studies, a library of derivatives was designed, synthesized and evaluated for BACE-1 inhibition in-vitro. The docking studies were performed on Glide (Schrodinger suite) and Molegro virtual docker. Theoretical toxicity was predicted using Osiris Property Explorer. The synthesized compounds were tested for BACE-1 inhibition using in vitro assay based on Fluorescence Resonance Energy Transfer technique. The percent inhibition was cal-culated as a measure of activity. Results: The designed compounds revealed strong interactions with the desired amino acids of BACE-1 active sites. The aromatic rings placed at the fourth and sixth position of the pyrimidine ring occupied S1 and S3 substrate-binding clefts while the amino group formed hydrogen bonding interactions with Asp32 and Asp228. In silico data ensured that the compounds were orally bioavailable and brain permeable. The in vitro testing showed that the compounds inhibited BACE-1 at 10μM concentration. Conclusion: Compounds substituted with m-benzyloxy on one aromatic ring and o,p-di-chloro on another aromatic ring displayed maximum BACE-1 inhibition. Compound 2.13A displayed high docking score and was found to be most potent with IC50 of 6.92μM. The series displayed a good correlation between the docking score and BACE-1 inhibition profile.

Photocatalytic synthesis of 2-amino-4,6-diarylpyrimidines using nanoTiO2

Photocatalytic synthesis of 2-amino-4,6-diarylpyrimidines was carried out by using nano TiO2. The method follows a green route by avoiding the use of toxic organic solvents and tedious experimental conditions. Compared with conventional methods the present strategy offers excellent yield under UV irradiation for a period of 20 min in ethanolic medium. Only a small quantity of nanocatalyst (1 mol%) is sufficient to achieve the completion of the reaction. The nanocatalyst can be reused up to four reaction cycles without much loss in the activity.

Secondary amines immobilized inside magnetic mesoporous materials as a recyclable basic and oxidative heterogeneous nanocatalyst for the synthesis of trisubstituted pyrimidine derivatives

A novel magnetic MCM-41 nanocomposite-based catalyst is reported for the first time in the multicomponent synthesis of trisubstituted pyrimidines in which piperazine is immobilized inside the mesochannels of magnetic MCM-41 as an organic base (α-Fe2

Synthesis, characterization, and anti-amoebic activity of N-(pyrimidin-2-yl)benzenesulfonamide derivatives

A new series of N-(pyrimidin-2-yl)benzenesulfonamide derivatives, 3a-3i and 4a-4i, was synthesized from pyrimidin-2-amines, 2a-2i, with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds

Synthesis of 2-amino-4,6-diarylpyrimidines using inorganic solid support under microwave and ultrasound irradiation and their antibacterial activity

An expeditious method for the exclusive one-pot synthesis of 2-amino-4,6-diarylpyrimidines (3a-i) is described by the condensation of variously substituted chalcones (1a-i) with guanidine nitrate using inorganic solid support under microwave or ultrasound

Efficient and facile three-component reaction for the synthesis of 2-amine-4,6-diarylpyrimidine under solvent-free conditions

An efficient and convenient multicomponent reaction for the preparation of 2-amine-4,6-diarylpyrimidine by aromatic aldehydes, aromatic ketones, and guanidine carbonate in the presence of sodium hydroxide under solvent-free conditions is reported. The sho

Synthesis and antituberculous activity of N-Mannich bases of 3-[4-(4-chlorophenyl)-6-(4-methylphenyl) pyrimidin-2-yl] iminoisatin derivatives

Isatin, its 5-chloro and 5-bromo derivatives have been reacted with 4-(4-cholorophenyl)-6-(4-methylphenyl)-2-aminopyrimidine to form Schiff bases and the N-Mannich bases of these compounds were synthesized by reacting them with formaldehyde and several se

Synthesis and antimicrobial activity of Schiff and Mannich bases of isatin and its derivatives with pyrimidine

Isatin and its derivatives have been reacted with 4-(4'-chlorophenyl)-6-(4''-methyl phenyl)-2-aminopyrimidine to form Schiff bases and the N-Mannich bases of these compounds were synthesized by reacting them with formaldehyde and several secondary amines.