Day: January 5, 2023

Transition-metal-free synthesis of pyrimidines from lignin β-O-4 segments via a one-pot multi-component reaction was written by Zhang, Bo;Guo, Tenglong;Li, Zhewei;Kuhn, Fritz E.;Lei, Ming;Zhao, Zongbao K.;Xiao, Jianliang;Zhang, Jian;Xu, Dezhu;Zhang, Tao;Li, Changzhi. And the article was included in Nature Communications in 2022.Name: 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

In this work, the synthesis of pyrimidines from lignin β-O-4 model compounds, the most abundant segment in lignin, mediated by NaOH through a one-pot multi-component cascade reaction is reported. Mechanism study suggests that the transformation starts by NaOH-induced deprotonation of Cα-H bond in β-O-4 model compounds, and involves highly coupled sequential cleavage of C-O bonds, alc. dehydrogenation, aldol condensation, and dehydrogenative aromatization. This strategy features transition-metal free catalysis, a sustainable universal approach, no need of external oxidant/reductant, and an efficient one-pot process, thus providing an unprecedented opportunity for N-containing aromatic heterocyclic compounds synthesis from biorenewable feedstock. With this protocol, an important marine alkaloid meridianin derivative can be synthesized, emphasizing the application feasibility in pharmaceutical synthesis. 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. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. 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.Name: 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of 1-Methyl-1H-imidazole Derivatives as Potent Jak2 Inhibitors was written by Su, Qibin;Ioannidis, Stephanos;Chuaqui, Claudio;Almeida, Lynsie;Alimzhanov, Marat;Bebernitz, Geraldine;Bell, Kirsten;Block, Michael;Howard, Tina;Huang, Shan;Huszar, Dennis;Read, Jon A.;Rivard Costa, Caroline;Shi, Jie;Su, Mei;Ye, Minwei;Zinda, Michael. And the article was included in Journal of Medicinal Chemistry in 2014.Related Products of 35265-83-9 This article mentions the following:

Structure based design, synthesis, and biol. evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clin. candidate AZD1480 (I), optimization of the series led to the discovery of compound II, a potent, orally bioavailable Jak2 inhibitor. Compound II displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound II demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9Related Products of 35265-83-9).

2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9) 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.Related Products of 35265-83-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

RAF inhibitors that evade paradoxical MAPK pathway activation was written by Zhang, Chao;Spevak, Wayne;Zhang, Ying;Burton, Elizabeth A.;Ma, Yan;Habets, Gaston;Zhang, Jiazhong;Lin, Jack;Ewing, Todd;Matusow, Bernice;Tsang, Garson;Marimuthu, Adhirai;Cho, Hanna;Wu, Guoxian;Wang, Weiru;Fong, Daniel;Nguyen, Hoa;Shi, Songyuan;Womack, Patrick;Nespi, Marika;Shellooe, Rafe;Carias, Heidi;Powell, Ben;Light, Emily;Sanftner, Laura;Walters, Jason;Tsai, James;West, Brian L.;Visor, Gary;Rezaei, Hamid;Lin, Paul S.;Nolop, Keith;Ibrahim, Prabha N.;Hirth, Peter;Bollag, Gideon. And the article was included in Nature (London, United Kingdom) in 2015.SDS of cas: 1375301-91-9 This article mentions the following:

Oncogenic activation of BRAF fuels cancer growth by constitutively promoting RAS-independent mitogen-activated protein kinase (MAPK) pathway signalling. Accordingly, RAF inhibitors have brought substantially improved personalized treatment of metastatic melanoma. However, these targeted agents have also revealed an unexpected consequence: stimulated growth of certain cancers. Structurally diverse ATP-competitive RAF inhibitors can either inhibit or paradoxically activate the MAPK pathway, depending whether activation is by BRAF mutation or by an upstream event, such as RAS mutation or receptor tyrosine kinase activation. Here we have identified next-generation RAF inhibitors (dubbed ‘paradox breakers’) that suppress mutant BRAF cells without activating the MAPK pathway in cells bearing upstream activation. In cells that express the same HRAS mutation prevalent in squamous tumors from patients treated with RAF inhibitors, the first-generation RAF inhibitor vemurafenib stimulated in vitro and in vivo growth and induced expression of MAPK pathway response genes; by contrast the paradox breakers PLX7904 and PLX8394 had no effect. Paradox breakers also overcame several known mechanisms of resistance to first-generation RAF inhibitors. Dissociating MAPK pathway inhibition from paradoxical activation might yield both improved safety and more durable efficacy than first-generation RAF inhibitors, a concept currently undergoing human clin. evaluation with PLX8394. In the experiment, the researchers used many compounds, for example, 2-Cyclopropyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine (cas: 1375301-91-9SDS of cas: 1375301-91-9).

2-Cyclopropyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine (cas: 1375301-91-9) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. 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.SDS of cas: 1375301-91-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Multiresidue determination of antibiotics in ready-to-eat duck eggs marketed through e-commerce stores in China and subsequent assessment of dietary risks to consumers was written by Ji, Xiaofeng;Xu, Yan;Wang, Jianmei;Lyu, Wentao;Li, Rui;Tan, Simin;Xiao, Yingping;Tang, Biao;Yang, Hua;Qian, Mingrong. And the article was included in Journal of Food Science in 2021.Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

In this work, the occurrence of 34 common antibiotic (15 sulfonamides and 19 quinolones) residues were evaluated in 236 ready-to-eat duck eggs (salted and preserved duck eggs) marketed through e-commerce stores by ultra-performance liquid chromatog. coupled to tandem mass spectrometry, and subsequent dietary risk assessments for Chinese consumers were conducted. Among violated positives in duck egg samples, 11 analytes were found including sulfamethazine, sulfaquinoxaline, sulfamethoxazole, sulfadiazine, sulfamonomethoxine, ciprofloxacin, enrofloxacin, ofloxacin, flumequine, sarafloxacin, and nalidixic acid. A higher number of antibiotics were detected in salted duck eggs (five sulfonamides and six quinolones) than in preserved duck eggs (one sulfonamide and two quinolones). The maximum contamination of sulfonamides and quniolones was 448.0μg/kg (sulfaquinoxaline) and 563.7μg/kg (enrofloxacin) in salted duck eggs, resp. Dietary exposure was evaluated through the estimated daily intake (EDI) of risky antibiotics (sulfamethazine, ciprofloxacin, and enrofloxacin) and hazard quotients (HQs). The results showed that EDIs and HQs were in the range of 0.0004 to 0.0099μg/kg bw/day and 0.0009 to 0.1594%, resp. The risk was low since HQs obtained were less than 100%. However, a special attention should be paid to ready-to-eat duck egg products high percentile consumers with the prosperity of e-commerce market in China. The present anal. method could be used for multiresidue determination of antibiotics in ready-to-eat duck eggs, and dietary risk assessments of risky antibiotics provided a support for the work of regulatory bodies to conduct surveillance programs regarding food safety evaluation of ready-to-eat foods. 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. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of pyrido[2,3-d]pyrimidinones by the reaction of aminopyrimidin-4-ones with benzylidene Meldrum’s acid derivatives was written by Quiroga, Jairo;Hormaza, Angelina;Insuasty, Braulio;Nogueras, Manuel;Sanchez, Adolfo;Hanold, Norbert;Meier, Herbert. And the article was included in Journal of Heterocyclic Chemistry in 1997.Quality Control of 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one This article mentions the following:

A series of pyrido[2,3-d]pyrimidine-4,7-diones I (R¹ = MeS, MeO; R² = H, Me; R³ = H, Cl, NO₂) were prepared from 6-amino-4-pyrimidinones (II) and benzylidene Meldrum’s acid derivatives (III) by cyclization reactions in boiling nitrobenzene. The structure of I, determined by NMR measurements, reveals a selective orientation of II and III in the addition step. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Quality Control of 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Quality Control of 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reactions of β-sulfenyl α,β-unsaturated ketones with guanidine, amidines, and diamines was written by Nishio, Takehiko;Tokunaga, Tatsuhiro;Omote, Yoshimori. And the article was included in Journal of Heterocyclic Chemistry in 1985.SDS of cas: 40230-24-8 This article mentions the following:

Cyclocondensation of RCOCH:CR¹SR² (I, R = Ph, R¹ = Me, R² = Et; R = R¹ = Me, R² = Ph; R = R¹ = Ph, R² = Et) with R³C(:NH)NH₂ (R³ = NH₂, Me, Ph) gave pyrimidine derivatives in 14-76% yields. Cyclocondensation of I with ethylenediamine or o-(H₂N)₂C₆H₄ afforded 1,4-diazepines. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8SDS of cas: 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. 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.SDS of cas: 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Assessment of a specific sample cleanup for the multiresidue determination of veterinary drugs and pesticides in salmon using liquid chromatography/tandem mass spectrometry was written by Castilla-Fernandez, Delia;Moreno-Gonzalez, David;Bouza, Marcos;Saez-Gomez, Andrea;Ballesteros, Evaristo;Garcia-Reyes, Juan F.;Molina-Diaz, Antonio. And the article was included in Food Control in 2021.Related Products of 1220-83-3 This article mentions the following:

A novel sample treatment approach based on a modified QuEChERS method was evaluated for the simultaneous determination of veterinary drug and pesticide residues in salmon in this work. To improve the QuEChERS performance, Enhanced Matrix Removal-Lipid dSPE cleanup sorbent was evaluated for the first time for the simultaneous anal. of these organic contaminants in salmon samples. Due to this sorbent can effectively remove coextd. families of lipids. To cover a wide range of polarities, 65 pesticides and 41 veterinary drugs with log Kow ranging from -1.4 to 5.5 were selected. Extracts after cleanup were analyzed by ultra-high-performance liquid chromatog.-tandem mass spectrometry for analyte confirmation and quantitation. Outstanding results were obtained for both extraction efficiency and matrix removal. A negligible matrix effect was obtained for 57% of the studied compounds, whereas the rest presented a soft matrix effect. The recovery for spiked samples was in agreement with the current European Union recommendations for most compounds The rest of the parameters were also satisfactory, reaching quantification limits lower than 3.7μg kg-1 in all cases. The precision was better than 20% in all cases. Finally, the method performance was successfully demonstrated with 20 salmon samples, five of which contained pesticide or veterinary drug residues. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Related Products of 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Related Products of 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A C4N4 Diaminopyrimidine Fluorophore was written by Noda, Hidetoshi;Asada, Yasuko;Maruyama, Tatsuro;Takizawa, Naoki;Noda, Nobuo N.;Shibasaki, Masakatsu;Kumagai, Naoya. And the article was included in Chemistry – A European Journal in 2019.Computed Properties of C16H13N3 This article mentions the following:

A new scaffold for producing efficient organic fluorescent materials was identified: 2,5-diamino-4,6-diarylpyrimidine featuring a C4N4 elemental composition Single-step installation of two aryl groups at the 4,6-positions of the pyrimidine core delivered fluorescent organic materials in a modular fashion. A range of fluorescent compounds with distinct absorption/emission properties was readily accessed by changing the aromatic attachments. A generally high absorption coefficient and quantum yield were observed, including C4N4 derivatives that could fluoresce even in the solid state. The two amino groups at the 2,5-positions of the pyrimidine were essential for intense fluorescence with a large Stokes shift, which was corroborated by structural relaxation to a p-iminoquinone-like structure in the excited state. Besides live-cell imaging capabilities, fluorescent labeling of a protein involved in autophagy elucidated a new protein-protein interaction, supporting potential utility in bioimaging applications. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Computed Properties of C16H13N3).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Computed Properties of C16H13N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and biological research of 2-aryl-4-morpholino-6-triazolylpyrimidine derivatives as antitumor PI3K inhibitors was written by Yang, Xiu-li;Wang, Tian-cai;Lin, Sen;Fan, Hou-xing. And the article was included in Jingxi Huagong in 2014.Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine This article mentions the following:

In order to find more active antitumor PI3K inhibitors, pyrimidine-2,4-diol was used as raw material to go through chlorination by POCl₃, coupling with morpholine, then iodine generation, which was followed by Sonogashira coupling to remove the trimethylsilyl in order to get the triazolyl intermediate. Finally, the intermediate went through Suzuki coupling to give 2-aryl-4-morpholino-6-triazolylpyrimidine 14-27. Their structures were confirmed by ¹HNMR and LC-MS. The in vitro anti-proliferative activity assay against A2780 was carried out by MTT detection method, and the results showed that, at the test concentration of 10μmol/L, the compounds 14 and 25 were more potent than clin. candidates GDC-0941 and BEZ-235, the inhibition rate of which reached 76.7% and 77.2%, resp. Furthermore, the results of pharmacokinetic study suggested that compound 25 was desirable: t_1/2 = 3.2 h, and AUC_0-∞ was 34,193 (ng·h)/mL. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. 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.Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Impacts of farmland application of antibiotic-contaminated manures on the occurrence of antibiotic residues and antibiotic resistance genes in soil: A meta-analysis study was written by Zhang, Yu;Cheng, Dengmiao;Xie, Jun;Zhang, Yuting;Wan, Yu;Zhang, Yueqiang;Shi, Xiaojun. And the article was included in Chemosphere in 2022.Application of 1220-83-3 This article mentions the following:

Meta-anal. of 94 published studies was conducted to explore the impacts of farmland application of antibiotic-contaminated manures on antibiotic concentrations and ARG abundances in manure-amended soil. Forty-nine antibiotics were reported, in which chlortetracycline, oxytetracycline, doxycycline, tetracycline, enrofloxacin, ciprofloxacin and norfloxacin were the most prevalent and had relatively high concentrations The responses of ARG and mobile genetic element (MGE) abundances to farmland application of antibiotic-contaminated manures varied considerably under different management strategies and environmental settings. On average, compared to unamended treatments, farmland application of antibiotic-contaminated manures significantly increased the total ARG and MGE abundances by 591% and 351%, resp. (P < 0.05). Of all the included ARG classes, the largest increase was found for sulfonamide resistance genes (1121%), followed by aminoglycoside (852%) and tetracycline (763%) resistance genes. Correlation anal. suggested that soil organic carbon (SOC) was significantly neg. correlated with antibiotic concentrations in manured soil (P < 0.05) due to the formation of covalent bonds and nonextractable residues. Soil silt content was significantly pos. correlated with antibiotic concentration (P < 0.05), which was attributed to greater sorption capacities. The ARG abundances were significantly pos. correlated with soil silt content, antibiotic concentrations, mean annual temperature, SOC, MGEs and soil pH (P < 0.05), suggesting that changes in these factors may shape the ARG profiles. Collectively, these findings advanced our understanding of the occurrence of antibiotics and ARGs in manure-amended soil and potential factors affecting them and will contribute to better management of these contaminants in future agricultural production In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Application of 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Application of 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia