Category: 1827-27-6

Recommanded Product: 5-Amino-2-fluoropyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Solvent and substituent effects on fluorine-19 chemical shifts in some 5-substituted 2-fluoropyridines. Author is Giam, Choo-Seng; Lyle, James L..

The 19F NMR chem. shifts of several 5-substituted 2-fluoropyridines in 4 widely different solvents have been measured. The effects of solvents and substituents on the shifts paralleled those in the benzene series with certain modifications.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 5-Amino-2-fluoropyridine. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 18F-Labeled Pyrido[3,4-d]pyrimidine as an Effective Probe for Imaging of L858R Mutant Epidermal Growth Factor Receptor. Author is Kimura, Hiroyuki; Okuda, Haruka; Ishiguro, Masumi; Arimitsu, Kenji; Makino, Akira; Nishii, Ryuichi; Miyazaki, Anna; Yagi, Yusuke; Watanabe, Hiroyuki; Kawasaki, Ikuo; Ono, Masahiro; Saji, Hideo.

In non-small-cell lung carcinoma patients, L858R mutation of epidermal growth factor receptor (EGFR) are often found and mol. target therapy using EGFR tyrosine kinase inhibitors is effective for the patients. However, the treatment frequently develops drug resistance by secondary mutation, of which approx. 50% is a T790M mutation. Thus, the ability to predict whether EGFR will undergo secondary mutation is extremely important. We synthesized a novel radiofluorinated 4-(anilino)pyrido[3,4-d]pyrimidine derivative ([18F]APP-1) and evaluated its potential as a positron emission tomog. (PET) imaging probe to discriminate different tumor of mutation. EGFR inhibition assay, cell-uptake and biodistribution study showed that [18F]APP-1 binds specifically to the L858R mutant EGFR but not to the L858R/T790M mutant. Finally, PET imaging study using [18F]APP-1 with tumor-bearing mice, the H3255 tumor (L858R mutant) was more clearly visualized than the H1975 tumor (L858R/T790M mutant).

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 5-Amino-2-fluoropyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 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.

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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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

HPLC of Formula: 1827-27-6. 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 Solvent and substituent effects on fluorine-19 chemical shifts in some 5-substituted 2-fluoropyridines. Author is Giam, Choo-Seng; Lyle, James L..

The 19F NMR chem. shifts of several 5-substituted 2-fluoropyridines in 4 widely different solvents have been measured. The effects of solvents and substituents on the shifts paralleled those in the benzene series with certain modifications.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Electric Literature 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 Design, Synthesis, and Structure-Activity Relationship of Indole-3-glyoxylamide Libraries Possessing Highly Potent Activity in a Cell Line Model of Prion Disease. Author is Thompson, Mark J.; Borsenberger, Vinciane; Louth, Jennifer C.; Judd, Katie E.; Chen, Beining.

Transmissible spongiform encephalopathies (TSEs) are a family of invariably fatal neurodegenerative disorders for which no effective curative therapy currently exists. We report here the synthesis of a library of indole-3-glyoxylamides and their evaluation as potential antiprion agents. A number of compounds demonstrated submicromolar activity in a cell line model of prion disease together with a defined structure-activity relationship, permitting the design of more potent compounds that effected clearance of scrapie in the low nanomolar range. Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Asymmetric synthesis of heterocyclic chloroamines and aziridines by enantioselective protonation of catalytically generated enamines.Reference of 5-Amino-2-fluoropyridine.

We report a method for the synthesis of chiral vicinal chloroamines via asym. protonation of catalytically generated prochiral chloroenamines using chiral Bronsted acids. The process is highly enantioselective, with the origin of asymmetry and catalyst substituent effects elucidated by DFT calculations We show the utility of the method as an approach to the synthesis of a broad range of heterocycle-substituted aziridines by treatment of the chloroamines with base in a one-pot process, as well as the utility of the process to allow access to vicinal diamines.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Aromatic fluorine compounds. X. The 2,3- and 2,6-difluoropyridines》. Authors are Finger, G. C.; Starr, Laurence D.; Roe, Arthur; Link, William J..The article about the compound:5-Amino-2-fluoropyridinecas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F).Computed Properties of C5H5FN2. Through the article, more information about this compound (cas:1827-27-6) is conveyed.

cf. CA 54, 6713i. The preparation of difluoropyridines by the Schiemann reaction was investigated. 2-Amino-6-fluoropyridine, necessary for the synthesis of 2,6-difluoropyridine by the Schiemann reaction, was conveniently prepared by the Curtius degradation of 6-fluoropicolinic hydrazide and by the Hofmann reaction on 6-fluoropicolinamide. Since an α-fluorine on a pyridine nucleus is preferentially replaced by hydrazine when it is either adjacent to or opposite a carbomethoxy group, the hydrazides necessary for the synthesis of 3-amino-2- and 6-fluoropyridine could not be prepared These amines were prepared from the appropriate 2-fluoropyridinecarboxamide by the Hofmann reaction. The preparation of difluoropyridines was successful with two of the aminofluoropyridines and led to the following new compounds: 2,3-difluoro- and 2,6-difluoropyridine.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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 the article 《A Bulky and Electron-Rich N-Heterocyclic Carbene Palladium Complex (SIPr)Ph2Pd(cin)Cl: Highly Efficient and Versatile for Buchwald-Hartwig Amination of (Hetero)aryl Chlorides with (Hetero)aryl Amines at Room Temperature》. Keywords: heterocyclic carbene palladium complex catalyst preparation; substituted amine preparation; hetero aryl chloride amine Buchwald Hartwig amination palladium catalyst.They researched the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6 ).Reference of 5-Amino-2-fluoropyridine. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:1827-27-6) here.

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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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Related Products of 1827-27-6. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Soluble-type small-molecule CD4 mimics as HIV entry inhibitors. Author is Kobayakawa, Takuya; Konno, Kiju; Ohashi, Nami; Takahashi, Kohei; Masuda, Ami; Yoshimura, Kazuhisa; Harada, Shigeyoshi; Tamamura, Hirokazu.

Several small mol. CD4 mimics have been reported previously as HIV-1 entry inhibitors, which block the interaction between the Phe43 cavity of HIV-1 gp120 and the host CD4. Known CD4 mimics such as NBD-556 possess significant anti-HIV activity but are less soluble in water, perhaps due to their hydrophobic aromatic ring-containing structures. Compounds with a pyridinyl group in place of the Ph group in these mols. have been designed and synthesized in an attempt to increase the hydrophilicity. Some of these new CD4 mimics, containing a tetramethylpiperidine ring show significantly higher water solubility than NBD-556 and have high anti-HIV activity and synergistic anti-HIV activity with a neutralizing antibody. The CD4 mimic that has a cyclohexylpiperidine ring and a 6-fluoropyridin-3-yl ring has high anti-HIV activity and no significant cytotoxicity. The present results will be useful in the future design and development of novel soluble-type mol. CD4 mimics.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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 HDAC4 Inhibitors with Cyclic Linker and Non-hydroxamate Zinc Binding Group: Design, Synthesis, HDAC Screening and in vitro Cytotoxicity evaluation., published in 2021-07-13, which mentions a compound: 1827-27-6, mainly applied to HDAC inhibitor screening cytotoxicity cyclic linker nonhydroxamate zinc binding, Name: 5-Amino-2-fluoropyridine.

Recent evidences highlight the usefulness of small mol. (Histone deacetylase 4) HDAC4 inhibitors in the several preclin. paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non-hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) derivatives with pyridine as cyclic linker and TZD ring as zinc binding group was designed and screened in a panel of isoenzymes of HDACs, wherein the most potent compounds exhibiting HDAC4 IC50-values<5 μM were 5 v, 5 w, 5 y and 5 z (IC50=4.2±1 μM, 0.75±0.03 μM, 4.9±0.5 and 2.3±0.5 μM, resp.). The docking studies displayed the unique binding mode of this series of compound at active site of HDAC4, wherein TZD ring was indicated as zinc binding group. Further, 5 w and 5 y were found as the most potent antiproliferative agent in lymphoblastic leukemia (CCRF-CEM) and breast cancer MDA-MB-231 cells. Compound 5 y was found to induce the apoptosis and DNA fragmentation of CEM cells. The western blotting anal. of 5 y also showed the presence of cleaved caspases supporting their apoptotic nature. Further, Class IIa (HDAC4) selectivity of 5 y was also supported by western blotting observations, wherein 5 y caused the accumulation of acetylated H3 but not of acetylated Tubulin. Thus, our findings endorse the further investigation of this series of compounds for their potential as targeted cancer therapeutic agents. As far as I know, this compound(1827-27-6)Name: 5-Amino-2-fluoropyridine can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem