Category: 188577-68-6

Vasbinder, Melissa M.; Alimzhanov, Marat; Augustin, Martin; Bebernitz, Geraldine; Bell, Kirsten; Chuaqui, Claudio; Deegan, Tracy; Ferguson, Andrew D.; Goodwin, Kelly; Huszar, Dennis; Kawatkar, Aarti; Kawatkar, Sameer; Read, Jon; Shi, Jie; Steinbacher, Stefan; Steuber, Holger; Su, Qibin; Toader, Dorin; Wang, Haixia; Woessner, Richard; Wu, Allan; Ye, Minwei; Zinda, Michael published the artcile< Identification of azabenzimidazoles as potent JAK1 selective inhibitors>, Recommanded Product: 4,5-Dichloropyridin-2-amine, the main research area is azabenzimidazoles screening JAK1 selective inhibitor STAT3; Azabenzimidazoles; JAK selectivity; JAK1; JAK1 inhibitors.

We have identified a class of azabenzimidazoles as potent and selective JAK1 inhibitors. Investigations into the SAR are presented along with the structural features required to achieve selectivity for JAK1 vs. other JAK family members. An example from the series demonstrated highly selective inhibition of JAK1 vs. JAK2 and JAK3, along with inhibition of pSTAT3 in vivo, enabling it to serve as a JAK1 selective tool compound to further probe the biol. of JAK1 selective inhibitors.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug screening. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Recommanded Product: 4,5-Dichloropyridin-2-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pfefferkorn, Jeffrey A.; Lou, Jihong; Minich, Martha L.; Filipski, Kevin J.; He, Mingying; Zhou, Ru; Ahmed, Syed; Benbow, John; Perez, Angel-Guzman; Tu, Meihua; Litchfield, John; Sharma, Raman; Metzler, Karen; Bourbonais, Francis; Huang, Cong; Beebe, David A.; Oates, Peter J. published the artcile< Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle>, Name: 4,5-Dichloropyridin-2-amine, the main research area is aminopicoline carboxylic acid cyclization transamidation; sulfonyl pyridone preparation glucokinase activation antidiabetic human.

A promising area of novel anti-diabetic therapy involves identification of small mol. activators of the glucokinase enzyme to reduce blood glucose and normalize glucose stimulated insulin secretion. Herein, the identification and optimization of a series of 4-sulfonyl-2-pyridone, i.e. I, activators is reported. The activators were evaluated for in vitro biochem. activation and pharmacokinetic properties. As part of these efforts, a unique metabolic liability of the 4-sulfonyl-2-pyridone ring system was identified wherein this heterocycle readily undergoes conjugation with glutathione under non-enzymic conditions.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Name: 4,5-Dichloropyridin-2-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pfefferkorn, Jeffrey A.; Lou, Jihong; Minich, Martha L.; Filipski, Kevin J.; He, Mingying; Zhou, Ru; Ahmed, Syed; Benbow, John; Perez, Angel-Guzman; Tu, Meihua; Litchfield, John; Sharma, Raman; Metzler, Karen; Bourbonais, Francis; Huang, Cong; Beebe, David A.; Oates, Peter J. published the artcile< Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle>, Name: 4,5-Dichloropyridin-2-amine, the main research area is aminopicoline carboxylic acid cyclization transamidation; sulfonyl pyridone preparation glucokinase activation antidiabetic human.

A promising area of novel anti-diabetic therapy involves identification of small mol. activators of the glucokinase enzyme to reduce blood glucose and normalize glucose stimulated insulin secretion. Herein, the identification and optimization of a series of 4-sulfonyl-2-pyridone, i.e. I, activators is reported. The activators were evaluated for in vitro biochem. activation and pharmacokinetic properties. As part of these efforts, a unique metabolic liability of the 4-sulfonyl-2-pyridone ring system was identified wherein this heterocycle readily undergoes conjugation with glutathione under non-enzymic conditions.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Name: 4,5-Dichloropyridin-2-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xie, Dongsheng; Lu, Jun; Xie, Jin; Cui, Junjun; Li, Teng-Fei; Wang, Yan-Chao; Chen, Yuan; Gong, Nian; Li, Xin-Yan; Fu, Lei; Wang, Yong-Xiang published the artcile< Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent D-amino acid oxidase inhibitor>, Formula: C5H4Cl2N2, the main research area is chlorodihydro pyridopyrazine dione preparation amino acid oxidase inhibitor; 5-Azaquinoxaline-2,3-diones; 8-Chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione; Analgesic effects; D-amino acid oxidase; DAAO inhibitors.

A series of 5-azaquinoxaline-2,3-dione derivatives were synthesized and evaluated on D-amino acid oxidase (DAAO) inhibition as potential α-hydroxylactam-based inhibitors. The potent inhibitory activities in vitro suggested that 5-nitrogen could significantly enhance the binding affinity by strengthening relevant hydrogen bond interactions. The analgesic effects of intrathecal and systemic injection of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione, a representative mol. of 5-azaquinoxaline-2,3-dione, were investigated in rodents. This research not only confirmed the analgesic effect of the DAAO inhibitors but provided a new class of chem. entities with oral application potential for the treatment of chronic pain and morphine analgesic tolerance.

European Journal of Medicinal Chemistry published new progress about Analgesics. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Formula: C5H4Cl2N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Brendel, Matthias; Sakhare, Priyanka R.; Dahiya, Gaurav; Subramanian, Parthasarathi; Kaliappan, Krishna P. published the artcile< Serendipitous Synthesis of Pyridoquinazolinones via an Oxidative C-C Bond Cleavage>, Application In Synthesis of 188577-68-6, the main research area is serendipitous synthesis pyridoquinazolinone oxidative carbon carbon bond cleavage.

A direct one-pot copper-catalyzed oxidative C-C bond cleavage route to the synthesis of pyridoquinazolinones is described. This one-pot strategy involves a copper-catalyzed C-N coupling followed by concomitant C(sp3)-H oxidation and amidation via oxidative C-C bond cleavage under an O2 atmosphere to deliver the target mols. in high yields.

Journal of Organic Chemistry published new progress about Acetophenones Role: RCT (Reactant), RACT (Reactant or Reagent). 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Application In Synthesis of 188577-68-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sokolov, V. B.; Aksinenko, A. Yu. published the artcile< Fluorinated triazinones from hexafluoroacetone ethoxycarbonylimine>, SDS of cas: 188577-68-6, the main research area is hexafluoroacetone ethoxycarbonylimine cyclocondensation binucleophile; trifluoromethyltriazinone derivative preparation.

The behavior of hexafluoroacetone ethoxycarbonylimine in cyclocondensation with various binucleophiles of the amidine type, viz., amino derivatives of N- and N,S-heterocycles, was studied. A preparative method for the synthesis of previously unknown annelated 2,2-bis(trifluoromethyl)-1,3,5-triazinones was developed.

Russian Chemical Bulletin (Translation of Izvestiya Akademii Nauk, Seriya Khimicheskaya) published new progress about Cyclocondensation reaction. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, SDS of cas: 188577-68-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bavetsias, Vassilios; Large, Jonathan M.; Sun, Chongbo; Bouloc, Nathalie; Kosmopoulou, Magda; Matteucci, Mizio; Wilsher, Nicola E.; Martins, Vanessa; Reynisson, Johannes; Atrash, Butrus; Faisal, Amir; Urban, Frederique; Valenti, Melanie; Brandon, Alexis de Haven; Box, Gary; Raynaud, Florence I.; Workman, Paul; Eccles, Suzanne A.; Bayliss, Richard; Blagg, Julian; Linardopoulos, Spiros; McDonald, Edward published the artcile< Imidazo[4,5-b]pyridine Derivatives As Inhibitors of Aurora Kinases: Lead Optimization Studies toward the Identification of an Orally Bioavailable Preclinical Development Candidate>, Quality Control of 188577-68-6, the main research area is imidazopyridine derivative arsenic inhibitor Aurora kinase orally bioavailable development.

Lead optimization studies using an imidazo[4,5-b]pyridinylpiperazine as the starting point led to a new class of imidazo[4,5-b]pyridine-based inhibitors of Aurora kinases that possessed the 1-benzylpiperazinyl motif at the 7-position, and displayed favorable in vitro properties. Cocrystn. of Aurora-A with a morpholinylmethylphenylimidazopyridinyl chlorobenzyl piperazine (CCT137444) provided a clear understanding into the interactions of this novel class of inhibitors with the Aurora kinases. Subsequent physicochem. property refinement by the incorporation of solubilizing groups led to the identification of 3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)methyl)-5-methylisoxazole (CCT137690)(I) which is a potent inhibitor of Aurora kinases (Aurora-A IC50 = 0.015±0.003 μM, Aurora-B IC50 = 0.025 μM, Aurora-C IC50 = 0.019 μM). I is highly orally bioavailable, and in in vivo efficacy studies it inhibited the growth of SW620 colon carcinoma xenografts following oral administration with no observed toxicities as defined by body weight loss.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Quality Control of 188577-68-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gudmundsson, Kristjan S.; Hinkley, Jack M.; Brieger, Michael S.; Drach, John C.; Townsend, Leroy B. published the artcile< An improved large-scale synthesis of 2-amino-4-chloropyridine and its use for the convenient preparation of various polychlorinated 2-aminopyridines>, Category: pyridine-derivatives, the main research area is aminochloropyridine preparation chlorination; polychlorinated aminopyridine preparation; pyridine amino polychlorinated preparation.

An efficient large scale synthesis of 2-amino-4-chloropyridine (I) has been achieved through a modification of existing literature procedures. I was used to prepare the previously unreported 2-amino-4,5-dichloropyridine. The known 2-amino-3,4-dichloropyridine and 2-amino-3,4,5-trichloropyridine were prepared from I by new routes and in higher yields than previously reported.

Synthetic Communications published new progress about 188577-68-6. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Malhotra, Rajesh; Rarhi, Chhanda; Diveshkumar, K. V.; Bommisetti, P.; Pany, Sushree Prangya P.; Roy, Subho; Pradeepkumar, P. I.; Kundu, Mrinalkanti published the artcile< Pyridopyrimidinone Derivatives as ΙDNAG-Quadruplex-Stabilizing Agents: Design, Synthesis and Biophysical Studies>, HPLC of Formula: 188577-68-6, the main research area is pyridopyrimidinone preparation quadruplex DNA stabilizer.

With an aim to engineer drug-like properties, pyridopyrimidinone based selective G4 DNA stabilizing agents, e.g., I were designed, synthesized and further they were evaluated for G4 DNA recognition properties. CD melting studies revealed the preferential stabilization of parallel topol. of promoter c-MYC and c-KIT G4 DNAs by the ligands, especially compound I and 4-[7-chloro-3-methyl-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl]-N-(2-dimethylamino-ethyl)-benzamide, over the different topologies of telomeric G4 DNA. UV melting experiments suggested that no significant stabilization was observed for duplex DNA. Further, the results from ITC experiments substantiated the preferential stabilization of parallel topol. of c-MYC G4 DNA over telomeric and duplex DNA by the ligands I. These data showed that ligand I has moderate binding affinity to the c-MYC G4 DNA and is ~49-fold and ~25-fold selective over the telomeric G4 DNA and the duplex DNA resp. The mol. modeling and dynamics studies of the ligand I in complex with c-MYC and c-KIT1 G4 DNAs showed that this ligand stacks on the 5′-quartet of c-MYC and 3′-quartet of c-KIT1 G4 DNA structures.

ChemistrySelect published new progress about Circular dichroism. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, HPLC of Formula: 188577-68-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 188577-68-6, name is 4,5-Dichloropyridin-2-amine, the common compound, a new synthetic route is introduced below. Safety of 4,5-Dichloropyridin-2-amine

To a 50 ml round-bottomed flask containing 2-amino-4,5-dichloropyridine (0.275 g, 1.65 mmol) and cooled into an ice-bath was added conc. H2SO4 (2.79 g). The reaction mixture was stirred for 3 min and then HNO3 (70%; 0.186 g) was dropwise added. The reaction mixture was stirred at 0 C. (ice-bath) for 7 min, then heated to 55 C. and stirred at this temperature for 1 h, allowed to cool to room temperature, diluted with ice-water (15 ml) and the pH was adjusted to 7.5 with 10% aqueous NaOH. The yellow precipitate was collected by filtration, washed with water and dried in vacuo over P2O5, then absorbed on silica gel and the free running powder was placed on a 10 g isolute silica column. Elution with 2% ethyl acetate in dichloromethane afforded the title compound as a yellow solid (0.090 g, 26%); 1H-NMR (250 Mz, DMSO-d6) 7.39 (s, 2H, NH2), 8.39 (s, 1H, 6-H); LC-MS (ESI, m/z) 6.54 min-208, 210, 212 [(M+H)+, Cl2 isotopic pattern].

The synthetic route of 188577-68-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; THE INSTITUTE OF CANCER RESEARCH; US2009/247507; (2009); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem