Day: November 25, 2022

Wang, Guofang published the artcileDenitrogenative Pd/Cu-catalyzed Suzuki-type Cross-coupling of Aryltrifluoroborates with Arylhydrazine Hydrochlorides in Water under Room Temperature, Related Products of pyrazoles-derivatives, the publication is Applied Organometallic Chemistry (2018), 32(3), n/a, database is CAplus.

In the presence of Pd(NH₃)₂Cl₂ and CuCl₂ using K₂CO₃, potassium aryltrifluoroborates (and a styryltrifluoroborate) underwent green and aerobic denitrogenative coupling reactions with arylhydrazine monohydrochlorides in water to yield biaryls and trans-stilbene in 62-95% yields.

Applied Organometallic Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C10H18O, Related Products of pyrazoles-derivatives.

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

Patel, N. C. published the artcileSynthesis of bisazo disperse dyes based on 4-hydroxyl-1-phenylquinolin-2(1H)-one system and their dyeing performance on polyester fabric, Application In Synthesis of 14580-22-4, the publication is Journal of Indian Council of Chemists (2001), 18(1), 59-62, database is CAplus.

Ten 3-[4-(arylazo)phenylazo]-4-hydroxy-1-phenyl-2(1H)-quinolinone dyes were prepared by coupling diazotized 3-(4-aminophenylazo)-4-hydroxy-1-phenyl-2(1H)-quinolinone with various coupling components. 4-Hydroxy-1-phenyl-2(1H)-quinolinone (I) was prepared by the condensation of o-chlorobenzoic acid and aniline giving N-phenylanthranilic acid followed by acetylation giving N-acetyl-N-phenylanthranilic acid and ring closure. I was coupled with diazotized 4-aminoacetanilide giving a monoazo compound which on hydrolysis gave the diazo component for disazo dye preparation The dyes were characterized by elemental and spectral analyses and their dyeing performance on polyester fabric was assessed. The dyes when applied on polyester fabric gave shades with poor to good light fastness, very good to excellent wash fastness, and poor to excellent exhaustion.

Journal of Indian Council of Chemists published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Application In Synthesis of 14580-22-4.

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

Patel, N. C. published the artcileSynthesis and application of some bisazo disperse dyes based on 4-hydroxyquinolinoquinazoline system on polyester fabric, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Journal of Indian Council of Chemists (2001), 18(2), 83-86, database is CAplus.

Ten 3-(4′-R-azo-1′-phenylazo)-4-hydroxyquinolino-[1,2-b]-4-oxoquinazolines were prepared by coupling diazotized 3-(4′-amino-1′-phenylazo)-4-hydroxyquinolino-[1,2-b]-4-oxoquinazoline with various coupling components. 4-Hydroxyquinolino-[1,2-b]-4-oxoquinazoline (I) was prepared by the condensation of 2-methyl-1,3-benzoxazin-8-one with anthranilic acid, giving initially 2-methyl-3-(1-carboxyphenyl)-4-oxoquinazoline followed by the ring closure. I was coupled with diazotized p-aminoacetanilide followed by hydrolysis to give 3-[4′-amino-1′-phenylazo]-4-hydroxyqinolino[1,2-b]-4-oxoquinazoline. The bisazo disperse dyes were characterized by elemental and spectral analyses and their dyeing performance on polyester fabric was assessed. These compounds when applied on polyester fabric, gave shades with poor to good light fastness, very good to excellent wash fastness and poor to excellent exhaustion.

Journal of Indian Council of Chemists published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Cui, J. Jean published the artcileDiscovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the Treatment of Cancer, HPLC of Formula: 763120-58-7, the publication is Journal of Medicinal Chemistry (2012), 55(18), 8091-8109, database is CAplus and MEDLINE.

The c-MET receptor tyrosine kinase is an attractive oncol. target because of its critical role in human oncogenesis and tumor progression. An oxindole hydrazide hit 6 (VI) was identified during a c-MET HTS campaign and subsequently demonstrated to have an unusual degree of selectivity against a broad array of other kinases. The cocrystal structure of the related oxindole hydrazide c-MET inhibitor 10 (X) with a nonphosphorylated c-MET kinase domain revealed a unique binding mode associated with the exquisite selectivity profile. The chem. labile oxindole hydrazide scaffold was replaced with a chem. and metabolically stable triazolopyrazine scaffold using structure based drug design. Medicinal chem. lead optimization produced 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (2, II, PF-04217903), an extremely potent and exquisitely selective c-MET inhibitor. 2 Demonstrated effective tumor growth inhibition in c-MET dependent tumor models with good oral PK properties and an acceptable safety profile in preclin. studies. 2 Progressed to clin. evaluation in a Phase I oncol. setting.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, HPLC of Formula: 763120-58-7.

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

Margrey, Kaila A. published the artcilePredictive Model for Site-Selective Aryl and Heteroaryl C-H Functionalization via Organic Photoredox Catalysis, Quality Control of 930-36-9, the publication is Journal of the American Chemical Society (2017), 139(32), 11288-11299, database is CAplus and MEDLINE.

Direct C-H functionalization of aromatic compounds is a useful synthetic strategy that has garnered much attention because of its application to pharmaceuticals, agrochems., and late-stage functionalization reactions on complex mols. On the basis of previous methods disclosed by our lab, we sought to develop a predictive model for site selectivity and extend this aryl functionalization chem. to a selected set of heteroaromatic systems commonly used in the pharmaceutical industry. Using electron d. calculations, we were able to predict the site selectivity of direct C-H functionalization in a number of heterocycles and identify general trends observed across heterocycle classes.

Journal of the American Chemical Society published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Quality Control of 930-36-9.

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

Sandhu, Bhupinder published the artcileAssessment of computational tools for predicting supramolecular synthons, Quality Control of 3553-12-6, the publication is Chemistry (Basel, Switzerland) (2021), 3(2), 612-629, database is CAplus.

The ability to predict the most likely supramol. synthons in a crystalline solid is a valuable starting point for subsequently predicting the full crystal structure of a mol. with multiple competing mol. recognition sites. Energy and informatics-based prediction models based on mol. electrostatic potentials (MEPs), hydrogen-bond energies (HBE), hydrogen-bond propensity (HBP), and hydrogen-bond coordination (HBC) were applied to the crystal structures of twelve pyrazole-based mols. HBE, the most successful method, correctly predicted 100% of the exptl. observed primary intermol.-interactions, followed by HBP (87.5%), and HBC = MEPs (62.5%). A further HBC anal. suggested a risk of synthon crossover and synthon polymorphism in mols. with multiple binding sites. These easy-to-use models (based on just 2-D chem. structure) can offer a valuable risk assessment of potential formulation challenges.

Chemistry (Basel, Switzerland) published new progress about 3553-12-6. 3553-12-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Amide, name is 3-Acetamidopyrazole, and the molecular formula is C5H7N3O, Quality Control of 3553-12-6.

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

Matthews, Thomas P. published the artcileDesign and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases, SDS of cas: 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(14), 4045-4049, database is CAplus and MEDLINE.

A range of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazine ATP-competitive inhibitors, e.g. I and II, of CHK1 were developed by scaffold hopping from a weakly active screening hit. Efficient synthetic routes for parallel synthesis were developed to prepare analogs with improved potency and ligand efficiency against CHK1. Kinase profiling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases, including CHK2 and ABL, with equivalent or better potency depending on the pendant substitution. These 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines appear to represent a general kinase inhibitor scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, SDS of cas: 763120-58-7.

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

Matthews, Thomas P. published the artcileDesign and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases, Quality Control of 724710-02-5, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(14), 4045-4049, database is CAplus and MEDLINE.

A range of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazine ATP-competitive inhibitors, e.g. I and II, of CHK1 were developed by scaffold hopping from a weakly active screening hit. Efficient synthetic routes for parallel synthesis were developed to prepare analogs with improved potency and ligand efficiency against CHK1. Kinase profiling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases, including CHK2 and ABL, with equivalent or better potency depending on the pendant substitution. These 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines appear to represent a general kinase inhibitor scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Quality Control of 724710-02-5.

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

Hanna, Samer J. published the artcileThe Role of Rho-GTPases and actin polymerization during Macrophage Tunneling Nanotube Biogenesis, Recommanded Product: 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Scientific Reports (2017), 7(1), 1-16, database is CAplus and MEDLINE.

Macrophage interactions with other cells, either locally or at distances, are imperative in both normal and pathol. conditions. While soluble means of communication can transmit signals between different cells, it does not account for all long distance macrophage interactions. Recently described tunneling nanotubes (TNTs) are membranous channels that connect cells together and allow for transfer of signals, vesicles, and organelles. However, very little is known about the mechanism by which these structures are formed. Here we investigated the signaling pathways involved in TNT formation by macrophages using multiple imaging techniques including super-resolution microscopy (3D-SIM) and live-cell imaging including the use of FRET-based Rho GTPase biosensors. We found that formation of TNTs required the activity and differential localization of Cdc42 and Rac1. The downstream Rho GTPase effectors mediating actin polymerization through Arp2/3 nucleation, Wiskott-Aldrich syndrome protein (WASP) and WASP family verprolin-homologous 2 (WAVE2) proteins are also important, and both pathways act together during TNT biogenesis. Finally, TNT function as measured by transfer of cellular material between cells was reduced following depletion of a single factor demonstrating the importance of these factors in TNTs. Given that the characterization of TNT formation is still unclear in the field; this study provides new insights and would enhance the understanding of TNT formation towards investigating new markers.

Scientific Reports published new progress about 71203-35-5. 71203-35-5 belongs to pyrazoles-derivatives, auxiliary class GPCR/G Protein,Ras, name is 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C22H21N3O3S, Recommanded Product: 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide.

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

Turanov, Alexander N. published the artcileTripodal organophosphorus ligands as synergistic agents in the solvent extraction of lanthanides(III). Structure of mixed complexes and effect of diluents, Computed Properties of 4551-69-3, the publication is Polyhedron (2019), 276-288, database is CAplus.

The solvent extraction of lanthanides (III) (except for Pm) from chloride medium (at μ = 0.1) into an organic phase containing 4-benzoyl-3-methyl-1-phenyl-5-pyrazolone (HPy) and neutral tripodal ligands on the triphenylphosphine oxide platform with anchored carbamoyl side arms (2-R₂NC(O)CH₂OC₆H₄)₃PO, where R = Bu (L1) and cyclo-Hex (L2) has been studied. A considerable synergistic effect (up to 10⁷) has been observed in the presence of neutral ligands L1 or L2 in the organic phase containing HPy. The stoichiometry of the Ln(III) extracted species has been determined by slope anal. and the equilibrium constants have been calculated It has been found that the lanthanides(III) ions are extracted with mixtures of HPy and neutral ligands L1 or L2 in toluene as LnPy₃L species. The [LaPy₃(H₂O)₂], and new [LaPy₃(L1)] and [LaPy₃(L2)] complexes have been synthesized and characterized via elemental anal. and IR spectroscopy. Solution structure of the above complexes has been examined by IR and multinuclear (¹H, ¹³C, and ³¹P) NMR spectroscopy in toluene-d₈ and CDCl₃. The effect of diluents on synergistic extraction and the solution structure of mixed complexes are discussed.

Polyhedron published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C11H14O2, Computed Properties of 4551-69-3.

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