Category: 1827-27-6

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 5-Amino-2-fluoropyridine(SMILESS: NC1=CN=C(C=C1)F,cas:1827-27-6) is researched.Quality Control of Nickel(II) bromide ethylene glycol dimethyl ether complex. The article 《Pyridyl-urea catalysts for the solvent-free ring-opening polymerization of lactones and trimethylene carbonate》 in relation to this compound, is published in European Polymer Journal. Let’s take a look at the latest research on this compound (cas:1827-27-6).

The ring-opening polymerization (ROP) of lactones is an effective method for the preparation of biocompatible and biodegradable aliphatic polyesters, for which the development of efficient organocatalysts with high activity and good controllability is highly desirable. A series of novel pyridyl-urea catalysts was synthesized and applied in the solvent-free ROP of lactones and trimethylene carbonate. Combined with 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD), the pyridyl-urea/MTBD systems showed a fast and living/controlled behavior in the ROP, generating polymers with narrow mol. weight distributions. The influences of catalyst structure, type of base, pyridyl-urea/base ratio, feed ratio of monomer/initiator and reaction temperature on the catalytic properties were investigated. A possible mechanism was proposed on the basis of NMR titration and dilution experiments

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Chitneni, Satish K.; Reitman, Zachary J.; Spicehandler, Rebecca; Gooden, David M.; Yan, Hai; Zalutsky, Michael R. published an article about the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F ).Product Details of 1827-27-6. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1827-27-6) through the article.

Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) are commonly found in gliomas. AGI-5198, a potent and selective inhibitor of the mutant IDH1 enzyme, was radiolabeled with radioiodine and fluorine-18. These radiotracers were evaluated as potential probes for imaging mutant IDH1 expression in tumors with positron emission tomog. (PET). Radioiodination of AGI-5198 was achieved using a tin precursor in 79±6% yield (n=9), and 18F-labeling was accomplished by the Ugi reaction in a decay-corrected radiochem. yield of 2.6±1.6% (n=5). The inhibitory potency of the analogous nonradioactive compounds against mutant IDH1 (IDH1-R132H) was determined in enzymic assays. Cell uptake studies using radiolabeled AGI-5198 analogs revealed somewhat higher uptake in IDH1-mutated cells than that in wild-type IDH1 cells. The radiolabeled compounds displayed favorable tissue distribution characteristics in vivo, and good initial uptake in IDH1-mutated tumor xenografts; however, tumor uptake decreased with time. Radioiodinated AGI-5198 exhibited higher tumor-to-background ratios compared with 18F-labeled AGI-5198; unfortunately, similar results were observed in wild-type IDH1 tumor xenografts as well, indicating lack of selectivity for mutant IDH1 for this tracer. These results suggest that AGI-5198 analogs are not a promising platform for radiotracer development. Nonetheless, insights gained from this study may help in design and optimization of novel chem. scaffolds for developing radiotracers for imaging the mutant IDH1 enzyme.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 1827-27-6, is researched, Molecular C5H5FN2, about Copper-Catalyzed Electrochemical C-H Amination of Arenes with Secondary Amines, the main research direction is copper catalyzed electrochem carbon hydrogen amination arene secondary amine.Electric Literature of C5H5FN2.

Electrochem. oxidation represents an environmentally friendly solution to conventional methods that require caustic stoichiometric chem. oxidants. However, C-H functionalizations merging transition-metal catalysis and electrochem. techniques are, to date, largely confined to the use of precious metals and divided cells. Herein, the authors report the 1st examples of Cu-catalyzed electrochem. C-H aminations of arenes at room temperature using undivided electrochem. cells, thereby providing a practical solution for the construction of arylamines. The use of Bu4NI as a redox mediator is crucial for this transformation. From mechanistic studies including kinetic profiles, isotope effects, cyclic voltammetric analyses, and radical inhibition experiments, the reaction appears to proceed via a single-electron-transfer (SET) process, and a high valent Cu(III) species is likely involved. These findings provide a new avenue for transition-metal-catalyzed electrochem. C-H functionalization reactions using redox mediators.

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Huang, Huazhang; Nishi, Kosuke; Tsai, Hsing-Ju; Hammock, Bruce D. published an article about the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F ).Application In Synthesis of 5-Amino-2-fluoropyridine. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1827-27-6) through the article.

Fatty acid amide hydrolase (FAAH) is a pharmaceutical target whose inhibition may lead to valuable therapeutics. Sensitive substrates for high-throughput assays are crucial for the rapid-screening FAAH inhibitors. Here we describe the development of novel and highly sensitive fluorescent assays for FAAH based on substituted aminopyridines. Examining the relationship between the structure and the fluorescence of substituted aminopyridines suggested that a methoxy group in the para position relative to the amino group in aminopyridines greatly increased the fluorescence (i.e., quantum yields approach unity). These novel fluorescent reporters had a high Stokes’ shift of 94 nm, and their fluorescence in buffer systems increased with pH values from neutral to basic. Fluorescent substrates with these reporters displayed a very low fluorescent background and high aqueous solubility Most importantly, fluorescent assays for FAAH based on these substrates were at least 25 times more sensitive than assays using related compounds with published colorimetric or fluorescent reporters. This property results in shorter assay times and decreased protein concentrations in the assays. Such sensitive assays will facilitate distinguishing the relative potency of powerful inhibitors of FAAH. When these fluorescent substrates were applied to human liver microsomes, results suggested that there was at least one amide hydrolase in addition to FAAH that could hydrolyze long-chain fatty acid amides. These results show that these fluorescent substrates are very valuable tools in FAAH activity assays including screening inhibitors by high-throughput assays instead of using the costly and labor-intensive radioactive ligands. Potential applications of novel fluorescent reporters are discussed.

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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Towards Property Profiling: SYNTHESIS and SAR Probing of New Tetracyclic Diazaphenothiazine Analogues, published in 2021, which mentions a compound: 1827-27-6, mainly applied to lung breast cancer SAR anticancer tertiary phenothiazine quinoline; antibacterial activity; antiproliferative activity; azaphenothiazines; lipophilicity; pharmacophore mapping; phenothiazine; similarity-activity landscape index, Related Products of 1827-27-6.

A series of new tertiary phenothiazine derivatives containing a quinoline and a pyridine fragment was synthesized by the reaction of 1-methyl-3-benzoylthio-4-butylthioquinolinium chloride with 3-aminopyridine derivatives bearing various substituents on the pyridine ring. The direction and mechanism of the cyclization reaction of intermediates with the structure of 1-methyl-4-(3-pyridyl)aminoquinolinium-3-thiolate was related to the substituents in the 2- and 4-pyridine position. The structures of the compounds were analyzed using 1H, 13C NMR (COSY, HSQC, HMBC) and X-ray anal., resp. Moreover, the antiproliferative activity against tumor cells (A549, T47D, SNB-19) and a normal cell line (NHDF) was tested. The antibacterial screening of all the compounds was conducted against the reference and quality control strain Staphylococcus aureus ATCC 29213, three clin. isolates of methicillin-resistant S. aureus (MRSA). In silico computation of the intermol. similarity was performed using principal component anal. (PCA) and hierarchical clustering anal. (HCA) on the pool of structure/property-related descriptors calculated for the novel tetracyclic diazaphenothiazine derivatives The distance-oriented property evaluation was correlated with the exptl. anticancer activities and empirical lipophilicity as well. The quant. shape-based comparison was conducted using the CoMSA method in order to indicate the potentially valid steric, electronic and lipophilic properties. Finally, the numerical sampling of similarity-related activity landscape (SALI) provided a subtle picture of the SAR trends.

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Formula: C5H5FN2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis and in vitro evaluation of [18F]BMS-754807: A potential PET ligand for IGF-1R. Author is Majo, Vattoly J.; Arango, Victoria; Simpson, Norman R.; Prabhakaran, Jaya; Kassir, Suham A.; Underwood, Mark D.; Bakalian, Mihran; Canoll, Peter; John Mann, J.; Dileep Kumar, J. S..

Radiosynthesis and in vitro evaluation of [18F](S)-1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide ([18F]BMS-754807 or [18F] I) a specific IGF-1R inhibitor was performed. [18F]I demonstrated specific binding in vitro to human cancer tissues. Synthesis of reference standard II(X= F) and corresponding bromo derivative II(X = X = Br), the precursor for radiolabeling were achieved from 2,4-dichloropyrrolo[2,1-f][1,2,4]triazine in three steps with 50% overall yield. The radioproduct was obtained in 8% yield by reacting 1a with [18F]TBAF in DMSO at 170 °C at high radiochem. purity and specific activity (1-2 Ci/μmol, N = 10). The proof of concept of IGF-IR imaging with [18F]I was demonstrated by in vitro autoradiog. studies using pathol. identified surgically removed grade IV glioblastoma, breast cancer and pancreatic tumor tissues. These studies indicate that [18F]I can be a potential PET tracer for monitoring IGF-1R.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Mukherjee, Paramita; Woroch, Cristian P.; Cleary, Leah; Rusznak, Mark; Franzese, Ryan W.; Reese, Matthew R.; Tucker, Joseph W.; Humphrey, John M.; Etuk, Sarah M.; Kwan, Sabrina C.; am Ende, Christopher W.; Ball, Nicholas D. researched the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6 ).Electric Literature of C5H5FN2.They published the article 《Sulfonamide Synthesis via Calcium Triflimide Activation of Sulfonyl Fluorides》 about this compound( cas:1827-27-6 ) in Organic Letters. Keywords: calcium triflimide sulfonyl fluoride amine nucleophilic addition; sulfonamide synthesis. We’ll tell you more about this compound (cas:1827-27-6).

A method using calcium triflimide [Ca(NTf2)2] as a Lewis acid to activate sulfonyl fluorides toward nucleophilic addition with amines is described. The reaction converts a wide array of sterically and electronically diverse sulfonyl fluorides and amines into the corresponding sulfonamides in good yield.

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Ouyang, Jia-Sheng; Liu, Siqi; Pan, Bendu; Zhang, Yaqi; Liang, Hao; Chen, Bin; He, Xiaobo; Chan, Wesley Ting Kwok; Chan, Albert S. C.; Sun, Tian-Yu; Wu, Yun-Dong; Qiu, Liqin published an article about the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F ).Application of 1827-27-6. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1827-27-6) through the article.

A bulky and electron-rich N-heterocyclic carbene palladium complex (SIPr)Ph2Pd(cin)Cl was synthesized and characterized. It was found to be highly efficient and versatile for the synthesis of substituted amines via coupling of different (hetero)aryl chlorides with various (hetero)aryl amines at room temperature, especially for the challenging amination of five- or six-membered ring heteroaryl chlorides with five- or six-membered ring heteroaryl amines. It was also successfully applied to the synthesis of various com. pharmaceuticals and candidate drugs or compounds with potential pharmacol. activities in high yields. All of these demonstrate its excellent catalytic efficacy in Buchwald-Hartwig amination and broad application prospects in relevant pharmaceutical preparations DFT calculations suggest that the steric-induced electronic interaction makes the ligand more electron-donating and the steric effect effectively regulates the rotation of iPr-Ph-iPr group in the catalyzed system due to the introduction of the di-Ph skeleton. Considering the electronic effect and steric effect together, the oxidative addition activation barriers by (SIPr)Ph2 and (SIPr) ligands are close to each other. The reductive elimination was the rate-determining step of (SIPr)Ph2Pd(cin)Cl-catalyzed system in the catalytic cycle, the appropriate steric hindrance of (SIPr)Ph2 ligand greatly reduces the energy barrier of this step. The perfect combination of electron-donating and steric hindrance ability of the ligand significantly improves the catalytic activity.

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Pyrazine – Wikipedia,
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Computed Properties of C5H5FN2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Copper-Catalyzed Electrochemical C-H Amination of Arenes with Secondary Amines. Author is Yang, Qi-Liang; Wang, Xiang-Yang; Lu, Jia-Yan; Zhang, Li-Pu; Fang, Ping; Mei, Tian-Sheng.

Electrochem. oxidation represents an environmentally friendly solution to conventional methods that require caustic stoichiometric chem. oxidants. However, C-H functionalizations merging transition-metal catalysis and electrochem. techniques are, to date, largely confined to the use of precious metals and divided cells. Herein, the authors report the 1st examples of Cu-catalyzed electrochem. C-H aminations of arenes at room temperature using undivided electrochem. cells, thereby providing a practical solution for the construction of arylamines. The use of Bu4NI as a redox mediator is crucial for this transformation. From mechanistic studies including kinetic profiles, isotope effects, cyclic voltammetric analyses, and radical inhibition experiments, the reaction appears to proceed via a single-electron-transfer (SET) process, and a high valent Cu(III) species is likely involved. These findings provide a new avenue for transition-metal-catalyzed electrochem. C-H functionalization reactions using redox mediators.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, European Journal of Medicinal Chemistry called Design, synthesis of novel celastrol derivatives and study on their antitumor growth through HIF-1α pathway, Author is Shang, Fan-Fan; Wang, Jing Ying; Xu, Qian; Deng, Hao; Guo, Hong-Yan; Jin, Xuejun; Li, Xiaoting; Shen, Qing-Kun; Quan, Zhe-Shan, which mentions a compound: 1827-27-6, SMILESS is NC1=CN=C(C=C1)F, Molecular C5H5FN2, Recommanded Product: 1827-27-6.

Four series of hypoxia-inducible factor-1 alpha (HIF-1α) functioning derivatives stemming from modifications to the C-29 carboxyl group of celastrol were designed and synthesized, and their anticancer activities were evaluated. To address the structure and activity relationship of each derivative, extensive structural changes were made. HRE luciferase reporter assay demonstrated that 12 modified compounds showed superior HIF-1α inhibitory activity. Among them, quinolin-7-yloxy derivative I exhibited the best features: first, it had the strongest HIF-1α inhibitory activity (IC50 = 0.05μM, 5-fold higher than that of celastrol), and second, it possessed lower cytotoxicity (22-fold lower, I 16.85μM vs. celastrol 0.76μM). Thus, the safety factor of C6 was about 112 times higher than that of celastrol. Western blot assay indicated that I may inhibit the expression of HIF-1α protein in cells. Addnl., I hindered tumor cell cloning, migration and induced cell apoptosis. It is worth mentioning that in the mouse tumor xenograft model, I (10 mg/kg) displayed good antitumor activity in vivo, showing a better inhibition rate (74.03%) than the reference compound 5-fluorouracil (inhibition rate, 59.58%). However, the celastrol treatment group experienced collective death after four doses of the drug. Moreover, I minimally affected the mouse weight, indicating that its application in vivo has little toxic effect. H&E staining experiments show that it could also exacerbate the degree of tumor cell damage. The results of water solubility experiment show that the solubility of I is increased by 1.36 times than that of celastrol. In conclusion, I is a promising antitumor agent through the HIF-1α pathway.

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