Month: January 2023

Nickel-catalyzed methylation of aryl halides/tosylates with methyl tosylate was written by Wang, Jiawang;Zhao, Jianhong;Gong, Hegui. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2017.Related Products of 257280-25-4 This article mentions the following:

This work describes the cross-electrophile methylation of aryl bromides and aryl tosylates with Me tosylate. The mild reaction conditions allow effective methylation of a wide set of heteroaryl electrophiles and dimethylation of dibromoarenes. In the experiment, the researchers used many compounds, for example, 5-Bromo-2-phenoxypyrimidine (cas: 257280-25-4Related Products of 257280-25-4).

5-Bromo-2-phenoxypyrimidine (cas: 257280-25-4) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Related Products of 257280-25-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Chemotherapy. XII. Some sulfanilamido heterocycles was written by Clark, J. H.;English, J. P.;Winnek, P. S.;Marson, H. W.;Cole, Q. P.;Clapp, J. W.. And the article was included in Journal of the American Chemical Society in 1946.Reference of 40230-24-8 This article mentions the following:

2-Sulfanilamido-4-methoxypyrimidine (I) (C.A. 36, 2532.9) (40 g.) in 400 cc. MeOH and 200 g. NH₃, heated at 110° for 1 h., gives 57% of 2-sulfanilamido-4-aminopyrimidine, m. 225-6° (m.ps. corrected) (C.A. 37, 1402.2). 2-Amino-4-methoxypyrimidine did not react with NH₃ under these conditions; at 200° for 4 h., 2,4-diaminopyrimidine is formed. I (8 g.) and 3.8 g. Et₂N(CH₂)₃NH₂, heated at 100-10° for 45 min., give 45% of 2-sulfanilamido-4-(3-diethylaminopropylamino)pyrimidine, m. 230-2°. Guanidine carbonate (II) (18 g.) and EtOCH₂COCH₂Ac, heated 4 h. on the steam bath, give 69% of 2-amino-4-ethoxymethyl-6-methylpyrimidine, m. 106-8°; the 2-sulfanilamido compound, m. 158-60°, 40%. II (25 g.) and 46.4 g. CH₂Bz₂, heated 3 h. at 180-210°, give 39% of 2-amino-4,6-diphenylpyrimidine, m. 135-7°; 2-sulfanilamido compound, m. 266-8°. The Na salt of 2,2-dimethyl-1,3-dioxolane-4-methanol in 200 cc. dioxane and 20 g. 2-amino-4-chloropyrimidine (extracted with the dioxane in a Soxhlet apparatus by refluxing overnight) give 70% of 2-amino-4-(2,2-dimethyl-1,3-dioxolan-4-ylmethoxy)pyrimidine, m. 105°; this yields 51% of the N⁴-Ac derivative, m. 249-51°, of the 2-sulfanilamido compound, m. 228-30°. II (50 g.), 43.2 g. of the Cu salt of 4,4-dimethyl-1,3-pentanedione, and 100 cc. EtOH, refluxed 1 h., the residue heated with stirring at 150-70° for 2 h., the cooled mass broken up under 500 cc. 1:4 HCl, the filtrate made basic with NH₄OH, and the precipitate refluxed with hexane, give 44% of 2-amino-4-tert-butylpyrimidine, m. 103-5.5°; the free ketone gives only 18%; 2-sulfanilamido compound, m. 236-7°, 45%; the N⁴-Ac derivative m. 248-51°, 63%. 2-Aminopyrimidine gives 50% of the N⁴-Ac derivative, m. 268°, of 2-(2-methylsulfanilamido)pyrimidine, m. 243-6°. II (10.6 g.) and 13.5 g. 3-methyl-2,4-pentanedione, heated at 150-60° for 1.5 h., give 65% of 2-amino-4,5,6-trimethylpyrimidine, m. 206-7°; 2-sulfanilamido compound, m. 242-4° (N⁴-Ac derivative, m. 286-8°). 2-Aminothiazole (100 g.), added to 200 cc. 20% oleum with cooling during 1 h., heated on a steam bath for 2 h., and poured into 450 cc. H₂O, give 69% of 2-amino-5(or 4)-thiazolesulfonic acid, m. 248° (analyzed as the Ba salt); 2-sulfanilamido comp., m. 258°. 2-Amino-4-methyl-5-thiazolesulfonic acid did not react with 4-AcNHC₆H₄SO₂Cl. H₂NNHCONH₂ (4.6 g.) and 12.7 g. EtO₂CCH₂COCl, heated at 60-70° for 30 min., give 37% of Et 2-amino-1,3,4-thiadiazole-5-acetate, m. 158-60°; coupling and hydrolysis give 2-sulfanilamido-1,3,4-thiadiazole-5-acetic acid, m. 209-12°. Et 2-amino-1,3,4-thiadiazole-5-butyrate, m. 153-4° (41%), yields 2-sulfanilamido-1,3,4-thiadiazole-5-butyric acid, m. 185.5-6.5°. Data are given for the maximum blood level (mg.-% following a single oral dose of 0.5 g. per kg.), bacteriostatic, and antimalarial activities. Only the tri-Me derivative approaches the activity of sulfadiazine in the bacteriostatic test; the extremely low relative activities of the others serve to point out that other factors in addition to the acidity of the compounds in question are important. Simple alkyl substitution of the pyrimidine ring or of the sulfanilamide nucleus does not markedly affect the maximum blood level as compared with sulfadiazine; more complicated substituents reduce this value somewhat; the value is still further reduced by amino substitution; the sulfonic acid group reduces the maximum blood level of sulfathiazole. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Reference of 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Reference of 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Direct Formic Acid Mediated Z-Selective Reductive Coupling of Dienes and Aldehydes was written by Cooze, Christopher;Dada, Raphael;Lundgren, Rylan J.. And the article was included in Angewandte Chemie, International Edition in 2019.Safety of 2-Methoxypyrimidine-5-carbaldehyde This article mentions the following:

Demonstrated was that formic acid mediated the Rh-catalyzed, Z-selective coupling of dienes and aldehydes. The processed was distinguished by broad tolerance towards reducible or electrophilic groups. Kinetic anal. suggested that generation of the catalytically active Rh intermediate by ligand dissociation was the rate-determining step. The rapid generation and trapping of Rh-allyl intermediates was key to preventing chain-walking isomerization events that plague related protocols. Insights gained through this study may have wider implications in selective metal-catalyzed hydrofunctionalization reactions. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Safety of 2-Methoxypyrimidine-5-carbaldehyde).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Safety of 2-Methoxypyrimidine-5-carbaldehyde

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Development and validation of a multiclass confirmatory method for the determination of over 60 antibiotics in eggs using liquid-chromatography high-resolution mass spectrometry was written by Paoletti, Fabiola;Sdogati, Stefano;Barola, Carolina;Giusepponi, Danilo;Moretti, Simone;Galarini, Roberta. And the article was included in Food Control in 2021.Category: pyrimidines This article mentions the following:

A multiclass method for the determination of antimicrobial substances in eggs has been developed and validated, covering sixty-three antibiotics belonging to ten families. After extraction with acidified acetonitrile and EDTA, the analytes were injected into a liquid-chromatog. high-resolution mass-spectrometry system operating in pos. ionization mode. The procedure was successfully validated as confirmatory method evaluating selectivity, linearity, precision, recovery, decision limit, detection capability, limits of detection and quantitation. The here developed is the first method including all the antibiotics with Maximum Residue Limit (MRL) in eggs, except very polar drugs (aminoglycosides and colistins), which require specific protocols. Finally, a wide survey was carried out analyzing 100 com. eggs samples from local markets. Only 3% contained residues of authorized substances at concentrations ower than the relevant MRLs. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Category: pyrimidines).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rapid and ultra-trace levels analysis of 33 antibiotics in water by on-line solid-phase extraction with ultra-performance liquid chromatography-tandem mass spectrometry was written by Shen, Fei;Xu, Yan-Juan;Wang, Ye;Chen, Jing;Wang, Shuo. And the article was included in Journal of Chromatography A in 2022.Recommanded Product: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

A method was developed for the determination of 33 antibiotics belonging to 4 different antibiotic groups, including sulfonamides (16), fluoroquinolones (12), macrolides (1), and tetracyclines (4) in water samples using online solid-phase extraction-ultra performance liquid chromatog.-electrospray ionization tandem mass spectrometry (online SPE-UPLC-MS/MS). The enrichment and anal. conditions were optimized for the determination of trace concentrations (nanogram per L). Aliquots of the water samples (5 mL) were filtered through a membrane and enriched on an online polymeric column with hydrophilic-lipophilic balance (HLB). The analyte was eluted by the mobile phase during online SPE and separated on an Acquity BEH130 column, detected by tandem mass spectrometry, and quantified using an external standard method. The optimization of the anal. methods was discussed, which included optimization of pH of the sample, filtration membrane, Na2EDTA, chromatog. column, formic acid and aqueous ammonia in mobile phase. The detection limit for all test compounds by this method was in the range of 0.2-1.5 ng/L, with recoveries of 76.6-118%. The precision of the method, as indicated by the relative standard deviation, was 2.4-7.9%. Results of anal. of surface water samples demonstrated the ability of the proposed method to analyze ultra-trace levels of antibiotics, without the need for complex manual pretreatment. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Recommanded Product: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Recommanded Product: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of Enantioenriched Allylic Silanes via Nickel-Catalyzed Reductive Cross-Coupling was written by Hofstra, Julie L.;Cherney, Alan H.;Ordner, Ciara M.;Reisman, Sarah E.. And the article was included in Journal of the American Chemical Society in 2018.Safety of 2-Methoxypyrimidine-5-carbaldehyde This article mentions the following:

An asym. Ni-catalyzed reductive cross-coupling has been developed to prepare enantioenriched allylic silanes. This enantioselective reductive alkenylation proceeds under mild conditions and exhibits good functional group tolerance. The chiral allylic silanes prepared here undergo a variety of stereospecific transformations, including intramol. Hosomi-Sakurai reactions, to set vicinal stereogenic centers with excellent transfer of chirality. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Safety of 2-Methoxypyrimidine-5-carbaldehyde).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Safety of 2-Methoxypyrimidine-5-carbaldehyde

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ag-Assisted Fluorination of Unprotected 4,6-Disubstituted 2-Aminopyrimidines with Selectfluor was written by Wang, Chenxi;Cai, Juewang;Zhang, Min;Zhao, Xiaoming. And the article was included in Journal of Organic Chemistry in 2017.COA of Formula: C16H13N3 This article mentions the following:

In the presence of Ag₂CO₃, arylpyrimidinamines I (R = Ph, 4-MeC₆H₄, 4-FC₆H₄; R¹ = PhCH₂, 4-MeC₆H₄CH₂, 4-FC₆H₄CH₂; R = R¹ = Ph, 4-FC₆H₄, 4-ClC₆H₄, 4-BrC₆H₄, 3-ClC₆H₄, 4-MeC₆H₄, 2-thienyl; R² = H) underwent regioselective fluorination with Selectfluor® in MeCN to yield 5-fluoro-2-pyrimidinamines I (R = Ph, 4-MeC₆H₄, 4-FC₆H₄; R¹ = PhCH₂, 4-MeC₆H₄CH₂, 4-FC₆H₄CH₂; R = R¹ = Ph, 4-FC₆H₄,4-ClC₆H₄, 4-BrC₆H₄, 3-ClC₆H₄, 4-MeC₆H₄, 2-thienyl; R² = F) in 44-72% yields. The structures of I (R = Ph; R¹ = PhCH₂; R² = F), I (R = R¹ = 2-thienyl; R² = F), and of the tetrasilver perchlorate complex of I (R = R¹ = Ph; R² = H) with Ph₂PCH₂PPh₂ were determined by X-ray crystallog. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8COA of Formula: C16H13N3).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.COA of Formula: C16H13N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Conversion of 2,4,6-triphenylpyrylium perchlorate to a pyrimidine series compound was written by Zhdanova, M. P.;Zvezdina, E. A.;Dorofeenko, G. N.. And the article was included in Khimiya Geterotsiklicheskikh Soedinenii in 1975.Name: 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

Pyrimidinylpyridinium perchlorate (I) was prepared in 63% yield by boiling pyrylium perchlorate (II) with guanidine 20 min in absolute DMF. Treatment of II with 2-amino-4,6-diphenylpyrimidine gave 94% I which confirmed its structure. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Name: 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Name: 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A tiered probabilistic approach to assess antibiotic ecological and resistance development risks in the fresh surface waters of China was written by Zhang, Jiawei;Ge, Hui;Shi, Jianghong;Tao, Huanyu;Li, Bin;Yu, Xiangyi;Zhang, Mengtao;Xu, Zonglin;Xiao, Ruijie;Li, Xiaoyan. And the article was included in Ecotoxicology and Environmental Safety in 2022.Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

Exposure to antibiotics can result in not only ecotoxicity on aquatic organisms but also the development of antibiotic resistance. In the study, the ecotoxicity data and min. inhibitory concentrations of the antibiotics were screened to derive predicted no-effect concentrations of ecol. (PNEC_eco) and resistance development risks (PNEC_res) for 36 antibiotics in fresh surface waters of China. The derived PNEC_eco and PNEC_res values were ranged from 0.00175 to 2351μg/L and 0.037-50μg/L, resp. Antibiotic ecol. and resistance development risks were geog. widespread, especially in the Yongding River, Daqing River, and Ziya River basins of China. Based on the risk quotients, 11 and 14 of 36 target antibiotics were at high ecol. risks and high resistance development risks in at least one basin, resp. The higher tiered assessments provided more detailed risk descriptions by probability values and β-lactams (penicillin and amoxicillin) were present at the highest levels for ecol. and resistance development risks. Although there was uncertainty based on the limited data and existing methods, this study can indicate the overall situation of the existing risk levels and provide essential insights and data supporting antibiotic management. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Effects of wastewater treatment and manure application on the dissemination of antimicrobial resistance around swine feedlots was written by Liu, Chong;Li, Xiaohua;Zheng, Shunan;Kai, Zhang;Jin, Tuo;Shi, Rongguang;Huang, Hongkun;Zheng, Xiangqun. And the article was included in Journal of Cleaner Production in 2021.Formula: C11H12N4O3S This article mentions the following:

China is the world’s largest swine producer and consumer of pork. The large amount of veterinary antibiotics used in swine production poses a significant environmental risk, and many wastewater treatment and manure application measures are taken to control the spread of antibiotic pollution from swine feedlots. However, the effectiveness of these measures in antibiotic and antibiotic resistance genes removal remains unclear. This study evaluated the fate of antibiotics and related resistance genes around 10 swine farms throughout China. A conventional wastewater treatment facility had limited ability to remove antibiotics and related resistance genes in effluent. Manure application increased the antibiotic concentration and related resistance genes abundance in agricultural soil, and simultaneously enhanced the correlation between class I integron and antibiotic resistance genes. Furthermore, the results revealed some factors such as heavy metals, dissolved oxygen and nutrients might play important roles in aggravating the antimicrobial resistance. The relevance network revealed that copper and zinc were significantly correlated with antibiotic resistance genes and class I/II integrons in manured soil and effluents from an anaerobic digester and membrane bioreactor, suggesting that excessive heavy metals could trigger co-selection and transfer of antibiotic resistance genes. Overall, the study revealed the risk of antibiotic residual and resistance gene pollution in swine wastewater treatment and manure application, highlighting the importance in the source control of antibiotic and heavy metal uses as well as the necessity to optimize wastewater treatment technol. for resistance removal. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Formula: C11H12N4O3S).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Formula: C11H12N4O3S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia