Tag: M.W=150-200

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. HPLC of Formula: 2927-71-1.

Zhao, Dan;Huang, Shanshan;Qu, Menghua;Wang, Changyuan;Liu, Zhihao;Li, Zhen;Peng, Jinyong;Liu, Kexin;Li, Yanxia;Ma, Xiaodong;Shu, Xiaohong research published 《 Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines》, the research content is summarized as follows. A new series of diphenylpyrimidine derivatives (DPPYs) bearing various aniline side chains at the C-2 position of pyrimidine core were synthesized as potent BTK inhibitors. Most of these inhibitors displayed improved activity against B leukemia cell lines compared with lead compound spebrutinib. Subsequent studies showed that the peculiar inhibitor I, with IC₅₀ values of 10.5 μM against Ramos cells and 19.1 μM against Raji cells, also displayed slightly higher inhibitory ability than the novel agent ibrutinib. Moreover, compound I is not sensitive to normal cells PBMC, indicating low cell cytotoxicity. In addition, flow cytometry anal. indicated that I significantly induced the apoptosis of Ramos cells, and arrested the cell cycle at the G0/G1 phase. These explorations provided new clues to discover pyrimidine scaffold as more effective BTK inhibitors.

HPLC of Formula: 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Synthetic Route of 2927-71-1.

Zhao, Qian;Manning, James R.;Sutton, James;Costales, Abran;Sendzik, Martin;Shafer, Cynthia M.;Levell, Julian R.;Liu, Gang;Caferro, Thomas;Cho, Young Shin;Palermo, Mark;Chenail, Gregg;Dooley, Julia;Villalba, Brian;Farsidjani, Ali;Chen, Jinyun;Dodd, Stephanie;Gould, Ty;Liang, Guiqing;Slocum, Kelly;Pu, Minying;Firestone, Brant;Growney, Joseph;Heimbach, Tycho;Pagliarini, Raymond research published 《 Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors》, the research content is summarized as follows. Mutant isocitrate dehydrogenase 1 (IDH1) is an attractive therapeutic target for the treatment of various cancers such as AML, glioma, and glioblastoma. The authors have evaluated 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant IDH1 inhibitors that bind to an allosteric, induced pocket of IDH1^R132H. This Letter describes SAR exploration focused on improving both the in vitro and in vivo metabolic stability of the compounds, leading to the identification of I as a potent and selective mutant IDH1 inhibitor that has demonstrated brain penetration and excellent oral bioavailability in rodents. In a preclin. patient-derived IDH1 mutant xenograft tumor model study, I efficiently inhibited the production of the biomarker 2-HG.

Synthetic Route of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Computed Properties of 65-86-1.

Zheng, Cheng;Miao, Rongxin;Liu, Yingmiao;Cao, Yang;Liu, Dong;Wang, Junzhi;Ying, Hanjie research published 《 A Procedure to Design One-Pot Multi-enzyme System for Industrial CDP-Choline Production》, the research content is summarized as follows. Abstract: Fermentation and chem. methods for industrial cytidine diphosphate choline (CDP-choline) catalytic production both suffer from several disadvantages such as relatively low efficiency and productivity. To overcome these problems, we applied the concept of synthetic biol. to develop a new one-pot multi-enzyme system to produce CDP-choline from orotic acid. Enzymes from different sources were selected and optimized as building blocks of the system, and parameters such as oxygen supply were also optimized. This system shows a titer of 37.6 ± 1.1 mM and a reaction rate of 1.6 mM L^-1 h^-1, both increase 66 % from traditional processes. It also has an efficiency of energy of 25.4%, improves 2-folds. This new one-pot CDP-choline-producing system has a potential for industrial use, and the procedure to design one-pot multi-enzyme system can be applied to build other one-pot system producing energy-rich compounds

65-86-1, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., Computed Properties of 65-86-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 4595-59-9, formula is C4H3BrN2, Name is 5-Bromopyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Recommanded Product: 5-Bromopyrimidine.

Zheng, Di-Zhong;Li, Dong-Hui;Liu, Huan;Shao, Youxiang;Ke, Zhuofeng;Liu, Feng-Shou research published 《 Bis(imino)acenaphthene (BIAN)-Supported N-Heterocyclic Carbene Palladium Complexes with Ancillary Ligands: Readily Activated Precatalysts for Direct C-H Arylation of Thiophenes》, the research content is summarized as follows. The authors report herein a highly efficient direct C-H arylation of thiophenes with (hetero)aryl bromides by bulky bis(imino)acenaphthene (BIAN)-supported N-heterocyclic carbene Pd complexes. The relation between the structure of Pd complexes with ancillary ligands and catalytic properties is discussed. Upon a low Pd loading of 0.01-0.05 mol %, the bulky Pd complex was successfully used to catalyze the cross-coupling of a variety of thiophenes with (hetero)aryl bromides under aerobic conditions. Also, it provides a practical and straightforward access to poly(3-hexylthiophenes) with high mol. weight and high HT value under aerobic reaction conditions. To access the mechanistic of the transformation, experiment study and DFT calculations on the direct arylation were performed, which supported the involvement of a Pd(0)/Pd(II) CMD process.

4595-59-9, 5-Bromopyrimidine is a reactive intermediate that is used in the synthesis of 4-methoxyphenylboronic acid. 5-Bromopyrimidine has been shown to be nucleophilic, reacting with β-amino acids under basic conditions to form the corresponding 2-bromo amide. It also undergoes cross-coupling reactions with halides and can be used as a building block for other organic compounds. 5-Bromopyrimidine has optical properties that are characteristic of aromatic molecules, including strong absorption bands in the ultraviolet region and visible light region.
5-Bromopyrimidine undergoes direct metallation with lithuium diisopropylamide to yield 4-lithio-5-bromopyrimidine., Recommanded Product: 5-Bromopyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Formula: C5H4N2O4.

Zhou, Yuan;Li, Ruoqi;Zheng, Yingyi;Song, Meiying;Zhang, Shanshan;Sun, Yunxia;Wei, Mengying;Fan, Xiang research published 《 Diosgenin ameliorates non-alcoholic fatty liver disease by modulating the gut microbiota and related lipid/ amino acid metabolism in high fat diet-fed rats》, the research content is summarized as follows. Non-alc. fatty liver disease (NAFLD) is a metabolic disease closely associated with dietary habits. Diosgenin is abundant in yam, a common food and traditional Chinese medicine. The mol. mechanism of diosgenin on NAFLD has been preliminarily explored. However, the effect of diosgenin on metabolism and gut microbiota in NAFLD has not been reported. This study confirmed that diosgenin could suppress excessive weight gain, reduce serum levels of total cholesterol and triglycerides, and decrease liver fat accumulation in high-fat diet-induced NAFLD rats. Moreover, fecal metabolomics anal. suggested diosgenin improved abnormal lipid and amino acid metabolism Bile acids, including lithocholic acid and ursodeoxycholic acid 3-sulfate that function as excretion, absorption, and transport of fats, were remarkably regulated by diosgenin. Aromatic amino acid and lysine metabolism was regulated by diosgenin as well. 16S rRNA gene sequencing anal. demonstrated that diosgenin restored gut microbiota disorder, especially Globicatella, Phascolarctobacterium, Pseudochrobactrum, and uncultured_bacterium_f_Prevotellaceae at the genus level. Addnl., these regulated bacterial genera showed significant correlations with lipid and amino acid metabolismrelated biomarkers. This study further confirmed the significant effect of diosgenin on NAFLD, and provided a new perspective for the mechanism.

65-86-1, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., Formula: C5H4N2O4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. COA of Formula: C5H4N2O4.

Zhu, Dan;Hayman, Alan;Frew, Russell;Kebede, Biniam;Chen, Gang;Stewart, Ian research published 《 Milk Powder Extraction: Optimization of Conditions for the Water-Soluble Metabolites by Proton Nuclear Magnetic Resonance (¹H-NMR)》, the research content is summarized as follows. Milk is a favorable for humans due to its nutritional composition Metabolites in milk relevant to human health have received increased attention. Proton NMR (¹H-NMR) is commonly used for water-soluble metabolites due to rapid data acquisition and excellent precision. Extraction to sep. fats and proteins from the metabolites is necessary to obtain high quality spectra. In the present work, various extraction procedures were compared for ¹H-NMR. The mass of milk for extraction was also optimized. Overall, 2/1 (volume/volume) methanol/skim milk was selected to be the most efficient system. The best precision was obtained for 500 to 600 mg milk powder redissolved in 2 mL water and 0.5 mL skim milk for the subsequent extraction This study provides a sample preparation protocol for milk metabolomics that may be appropriate for other samples.

COA of Formula: C5H4N2O4, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., 65-86-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. SDS of cas: 2927-71-1.

Zhu, Dancheng;Zheng, Kai;Qiao, Jun;Xu, Hao;Chen, Chao;Zhang, Pengfei;Shen, Chao research published 《 One-step synthesis of PdCu@Ti₃C₂ with high catalytic activity in the Suzuki-Miyaura coupling reaction》, the research content is summarized as follows. Owing to their enhanced catalytic stability and cyclability, two-dimensional (2D) material-supported Pd-based bimetallic alloys have promising applications for catalytic reactions. Furthermore, the alloying strategy can effectively reduce costs and improve catalytic performance. In this paper, we report a one-step reduction method to synthesize a novel heterogeneous catalyst, PdCu@Ti₃C₂, with good catalytic performance. The composition and structure of the as-prepared catalyst were characterized by inductively coupled plasma-mass spectrometry (ICP-MS), scanning transmission electron microscopy (STEM), energy-dispersive X-ray spectroscopy (EDX), and XPS. The catalyst particles, which were identified as a PdCu bimetallic alloy, exhibited good dispersion on the substrate. The performance of the catalyst in the Suzuki-Miyaura coupling reaction was studied, and the results showed that PdCu@Ti₃C₂ had excellent catalytic activity, similar to that of homogeneous Pd catalysts such as Pd(PPh₃)₄. Moreover, the prepared catalyst could be reused at least 10 times in the Suzuki-Miyaura coupling reaction with high yield.

SDS of cas: 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Recommanded Product: 2,4-Dichloro-5-fluoropyrimidine.

Zhang, Chufeng;Qi, Wenyan;Li, Yong;Tang, Minghai;Yang, Tao;Liu, Kongjun;Chen, Yong;Deng, Dexin;Xiang, Mingli;Chen, Lijuan research published 《 Discovery of 3-(4-(2-((1H-Indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1H-pyrazol-1-yl)propanenitrile Derivatives as Selective TYK2 Inhibitors for the Treatment of Inflammatory Bowel Disease》, the research content is summarized as follows. The design, synthesis, and structure-activity relationships (SARs) of 3-(4-(2-((1H-indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1H-pyrazol-1-yl)propanenitrile I [R⁵= 2-cyanoethyl; R⁶ = Me, fluoro; R⁷ = indolin-5-yl, 1-oxoisoindolin-5-yl, 1-tert-butoxycarbonylindol-5-yl, etc.] as selective TYK2 inhibitors was reported. Among them, compound I [R⁵ = 2-cyanoethyl; R⁶ = fluoro; R⁷ = 1-tert-butoxycarbonylindol-5-yl] exhibited acceptable TYK2 inhibition with an IC₅₀ value of 9 nM, showed satisfactory selectivity characteristics over the other three homologous JAK kinases, and performed good functional potency in the JAK/STAT signaling pathway on lymphocyte lines and human whole blood. In liver microsomal assay studied that the clearance rate and half-life of I [R⁵ = 2-cyanoethyl; R⁶ = fluoro; R⁷ = 1-tert-butoxycarbonylindol-5-yl] were 11.4 mL/min/g and 121.6 min, resp. Furthermore, in a dextran sulfate sodium colitis model, I [R⁵ = 2-cyanoethyl; R⁶ = fluoro; R⁷ = 1-tert-butoxycarbonylindol-5-yl] reduced the production of pro-inflammatory cytokines IL-6 and TNF-α and improved the inflammation symptoms of mucosal infiltration, thickening, and edema. Compound I [R⁵ = 2-cyanoethyl; R⁶ = fluoro; R⁷ = 1-tert-butoxycarbonylindol-5-yl] was aselective TYK2 inhibitor and was used to treat immune diseases and deserved further investigation.

Recommanded Product: 2,4-Dichloro-5-fluoropyrimidine, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 4595-59-9, formula is C4H3BrN2, Name is 5-Bromopyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Application of C4H3BrN2.

Zhang, Dawei;Gao, Xing;Min, Qiao-Qiao;Gu, Yucheng;Berthon, Guillaume;Zhang, Xingang research published 《 Coupling of Heteroaryl Halides with Chlorodifluoroacetamides and Chlorodifluoroacetate by Nickel Catalysis》, the research content is summarized as follows. A nickel-catalyzed cross-coupling of heteroaryl halides with chlorodifluoroacetamides and chlorodifluoroacetate was developed. The combination of NiCl₂ DME with 4,4′-diNon-bpy, co-ligand PPh₃, and additive LiCl renders the catalytic system efficient for the synthesis of medicinal interest heteroaryldifluoroacetamides. The application of the method leads to short and highly efficient synthesis of biol. active mols., providing a facile route for applications in medicinal chem. and agrochem.

Application of C4H3BrN2, 5-Bromopyrimidine is a reactive intermediate that is used in the synthesis of 4-methoxyphenylboronic acid. 5-Bromopyrimidine has been shown to be nucleophilic, reacting with β-amino acids under basic conditions to form the corresponding 2-bromo amide. It also undergoes cross-coupling reactions with halides and can be used as a building block for other organic compounds. 5-Bromopyrimidine has optical properties that are characteristic of aromatic molecules, including strong absorption bands in the ultraviolet region and visible light region.
5-Bromopyrimidine undergoes direct metallation with lithuium diisopropylamide to yield 4-lithio-5-bromopyrimidine., 4595-59-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Reference of 2927-71-1.

Zhang, Hongwang;Zhou, Longhu;Amichai, Sarah;Zandi, Keivan;Cox, Bryan;Schinazi, Raymond;Amblard, Franck research published 《 Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection》, the research content is summarized as follows. Exploration of the chem. space of known influenza polymerase PB2 inhibitor Pimodivir, was performed by our group. We synthesized and identified compounds I and II, two novel thienopyrimidine derivatives displaying anti-influenza A activity in the single digit nanomolar range in cell culture. Binding of these unique compounds in the influenza polymerase PB2 pocket was also determined using mol. modeling.

2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., Reference of 2927-71-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia