Category: 6313-54-8

Haga, Yuji published the artcileDiscovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist, Synthetic Route of 6313-54-8, the publication is Bioorganic & Medicinal Chemistry (2009), 17(19), 6971-6982, database is CAplus and MEDLINE.

A series of trans-3-oxospiro[(aza)isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide derivatives were synthesized to identify potent NPY Y5 receptor antagonists. Of the compounds, 21j (I)showed high Y5 binding affinity, metabolic stability and brain and cerebrospinal fluid (CSF) penetration, and low susceptibility to P-glycoprotein transporters. Oral administration of 21j significantly inhibited the Y5 agonist-induced food intake in rats with a min. ED of 1 mg/kg. This compound was selected for proof-of-concept studies in human clin. trials.

Bioorganic & Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Synthetic Route of 6313-54-8.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Charier, Sandrine published the artcilePhotophysics of a series of efficient fluorescent pH probes for dual-emission-wavelength measurements in aqueous solutions, Related Products of chlorides-buliding-blocks, the publication is Chemistry – A European Journal (2006), 12(4), 1097-1113, database is CAplus and MEDLINE.

This paper evaluates the 5-aryl-2-pyridyloxazole backbone to engineer donor-acceptor fluorescent pH probes after one- or two-photon absorption. Parent fluorophores, as well as derivatives that can be used to label biomols., can be easily obtained in good yields. These mols. exhibit a large one-photon absorption in the near-UV range, and a strong fluorescence emission that covers the whole visible domain. The 5-aryl-2-pyridyloxazole derivatives also possess significant cross sections for two-photon absorption. Upon pyridine protonation, large shifts were observed in the absorption spectra after one- and two-photon excitation, as well as in the emission spectra. This feature was used to measure the pK_a of the investigated compounds that range between 2 and 8. In most of the investigated derivatives, the pK_a increased upon light excitation and protonation exchanges took place during the lifetime of the excited state, as shown by phase-modulation fluorometry anal. Several 5-aryl-2-pyridyloxazole derivatives are suggested as efficient probes to reliably measure the pH of aqueous solutions by means of ratiometric methods that are dependent on fluorescence emission.

Chemistry – A European Journal published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Charier, Sandrine published the artcilepH sensors: An efficient fluorescent probe for ratiometric pH measurements in aqueous solutions, Safety of 2-Chloroisonicotinic acid, the publication is Angewandte Chemie, International Edition (2004), 43(36), 4785-4788, database is CAplus and MEDLINE.

Just a litmus paper changes from red to blue with an increase in pH, so the fluorescence emission of the oxazole derivative 1 shifts from green to blue. Ratiometric measurements of the fluorescence emissions of the two species, after one- or two-photon excitation, allow 1 to be employed as a pH sensor over the mid-pH range.

Angewandte Chemie, International Edition published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Safety of 2-Chloroisonicotinic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Somawardhana, C. W. published the artcileSynthesis of 2-[¹²³I and ¹²⁴I]-iodoisonicotinic acid hydrazide-potential radiotracers for tuberculosis, SDS of cas: 6313-54-8, the publication is Applied Radiation and Isotopes (1991), 42(3), 215-20, database is CAplus and MEDLINE.

The radiochem. syntheses of Me 2-[¹²³I]-iodoisonicotinate, 2-[¹²³I]-iodoisonicotinic acid hydrazide (I) and 2-[¹²⁴I]-iodoisonicotinic acid hydrazide was accomplished. Iodine-123 was incorporated in the Me ester mol. by an exchange reaction in glacial acetic acid. The average efficiency of iodine exchange reaction was (92.6%). This radiotracer was extracted with ether and the solvent was evaporated The residue was re-dissolved in anhydrous ethanol and treated with hydrazine under anhydrous conditions to obtain I. The overall radiochem. yield was 69%. Biodistribution data of both radio-tracers in male Sprague-Dawley rats were collected. This is the first report of SPECT radiopharmaceuticals which may be useful for differential diagnosis of intracranial masses (tuberculoma vs. glioma), and CNS tuberculosis in immunosuppressed subjects.

Applied Radiation and Isotopes published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C9H10O4, SDS of cas: 6313-54-8.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Ruiz Montoya, M. published the artcileA Contribution to the Elucidation of the Reduction Mechanism of 2-Chloroisonicotinic Acid on Mercury Electrodes, Recommanded Product: 2-Chloroisonicotinic acid, the publication is Journal of the Electrochemical Society (2008), 155(8), F190-F195, database is CAplus.

This paper presents polarog. (d.c. and differential pulse) and voltammetric (linear-sweep cyclic voltammetric) studies of the electroreduction of 2-chloroisonicotinic acid (2-chloro-4-pyridinecarboxylic acid), 2-CISO, at Hg electrodes. The dissociation constants of 2-CISO were obtained from the UV-visible absorption spectra (pK of 0.5 ± 0.03 corresponding to the -COOH group) and by potentiometric titration (pK of 3.46 corresponding to the protonation-dissociation of the heterocyclic N). The electrochem. studies were performed in the acidity range 2.7M H₂SO₄ to pH 7. Above the last pH value no signals were observed The overall reduction process involves the uptake of 4 electrons. Kinetics parameters such as Tafel slopes and electrochem. reaction orders were determined at potentials corresponding to the foot of the waves. A reaction mechanism can be proposed, consisting of an electrochem.-chem. process having 2 reversible electron transfers preceding a chem. step. At the scan rates used in cyclic voltammetry, the rate-determining step is the 2nd irreversible electron transfer. At pH°0.5 the recombination of the carboxylate anion with the H⁺ ion takes place prior to the reduction process.

Journal of the Electrochemical Society published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Recommanded Product: 2-Chloroisonicotinic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Duan, Maosheng published the artcileDiscovery of N-benzyl-N’-(4-piperidinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): Modification of the acyl portion, Application of 2-Chloroisonicotinic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(24), 7401-7404, database is CAplus and MEDLINE.

Modification of the acyl moiety in the CCR5 lead mol. 2 led to identification of several new classes of CCR5 antagonists. Antiviral activity and pharmacokinetic properties of the synthesized compounds were evaluated. Structure-activity relationship (SAR) derived from these studies further guided the optimization efforts, ultimately leading to the discovery of 36 (I) with an acceptable drug-like profile.

Bioorganic & Medicinal Chemistry Letters published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Application of 2-Chloroisonicotinic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Chen, Tiffany Q. published the artcileUnified Approach to Decarboxylative Halogenation of (Hetero)aryl Carboxylic Acids, Application In Synthesis of 6313-54-8, the publication is Journal of the American Chemical Society (2022), 144(18), 8296-8305, database is CAplus and MEDLINE.

A general catalytic method for direct decarboxylative halogenation of (hetero)aryl carboxylic acids RC(O)OH (R = 4-sulfamoylphenyl, 5-methylpyridin-2-yl, isoquinolin-1-yl, etc.) via ligand-to-metal charge transfer was reported. This strategy accommodates an exceptionally broad scope of substrates. An aryl radical intermediate is leveraged toward divergent functionalization pathways: (1) atom transfer to access bromo- or iodo(hetero)arenes or (2) radical capture by copper and subsequent reductive elimination to generate chloro- or fluoro(hetero)arenes. The proposed ligand-to-metal charge transfer mechanism is supported through an array of spectroscopic studies.

Journal of the American Chemical Society published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Application In Synthesis of 6313-54-8.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Xu, Shengtao published the artcileSynthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives, Related Products of chlorides-buliding-blocks, the publication is Fitoterapia (2014), 300-306, database is CAplus and MEDLINE.

A series of enmein-type derivatives were synthesized and assayed for their antimycobacterial effects. The structures of the synthesized compounds were established by ¹H NMR, ¹³C NMR and mass spectral anal. All the compounds were screened for their antimycobacterial properties against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Compounds 2, 6g and 6i were found to exhibit potent antimycobacterial activity against M. phlei at a concentration of 0.5 μg/mL, which was comparable to that of pos. drug streptomycin. Furthermore, five compounds were tested against Mycobacterium tuberculosis H₃₇Rv based on the promising preliminary screening results. Among them, compound 10 showed potent activity with IC₅₀ value of 17.1 μg/mL against M. tuberculosis H₃₇Rv strain. Thus, compound 10 could emerge as a promising lead for further research work.

Fitoterapia published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C19H17N3O, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Liu, Yang published the artcileDiscovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors, COA of Formula: C6H4ClNO2, the publication is European Journal of Medicinal Chemistry (2017), 122-132, database is CAplus and MEDLINE.

FGF receptors (FGFRs) are tyrosine kinases that are overexpressed in diverse tumors by genetic alterations such as gene amplifications, somatic mutations and translocations. Owing to this characteristic, FGFRs are attractive targets for cancer treatment. It has been demonstrated that most multi-targeted, ATP competitive tyrosine kinase inhibitors are active against FGFRs as well as other kinases. The design of new and more selective inhibitors of FGFRs, which might be reduced off-target and side effects, is a difficult yet significant challenge. The results of the current investigation, show that novel Ponatinib analogs are highly active as FGFR inhibitors and that they possess reduced kinase insert domain receptor (KDR) activities. Observations made in a structure and activity relationship (SAR) investigation led to the development of a promising, orally available lead compound 4-chloro-N-(4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) phenyl)-3-((5-morpholinopyridin-3-yl) ethynyl) benzamide (compound 4, I), which displays a 50-100-fold in vitro selectivity for inhibition of FGFR1-3 over KDR. In addition, biol. evaluation of I showed that it displays significant antitumor activities in FGFR1-amplificated H1581 and FGFR2-amplificated SNU-16 xenograft models.

European Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, COA of Formula: C6H4ClNO2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Liu, Jianbo published the artcileSynthesis of N-trifluoromethyl amides from carboxylic acids, Recommanded Product: 2-Chloroisonicotinic acid, the publication is Chem (2021), 7(8), 2245-2255, database is CAplus and MEDLINE.

Here, the synthesis of N-trifluoromethyl amides R¹C(O)NCF₃(R²) [R¹ = Et, cyclohexyl, CH₂CH₂Ph, etc.; R² = Me, allyl, CH₂CH₂Ph, etc.] from carboxylic acid halides and esters under mild conditions via isothiocyanates in the presence of silver fluoride at room temperature was reported. Through this strategy, isothiocyanates were desulfurized with AgF, and then the formed derivative was acylated to afford N-trifluoromethyl amides, including previously inaccessible structures. This method showed broad scope, provides a platform for rapidly generating N-trifluoromethyl amides by virtue of the diversity and availability of both reaction partners and should find application in the modification of advanced intermediates.

Chem published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Recommanded Product: 2-Chloroisonicotinic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics