Tag: M.W=200-250

Sap, Jeroen B. I. published the artcileSynthesis of ¹⁸F-difluoromethylarenes using arylboronic acids, ethyl bromofluoroacetate and [¹⁸F]fluoride, Safety of 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid, the publication is Chemical Science (2019), 10(11), 3237-3241, database is CAplus and MEDLINE.

Herein, the radiosynthesis of ¹⁸F-difluoromethylarenes RCHF¹⁸F (R = 4-C₂H₅, 4-OC₆H₅, 3,5-CH₃, etc.) via the assembly of three components, a boron reagent, Et bromofluoroacetate, and cyclotron-produced non-carrier added [¹⁸F]fluoride was reported. The two key steps are a copper-catalyzed cross-coupling reaction, and a Mn-mediated ¹⁸F-fluorodecarboxylation.

Chemical Science published new progress about 1025735-46-9. 1025735-46-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Benzene,Boronic Acids, name is 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid, and the molecular formula is C11H13BN2O2, Safety of 3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenylboronic acid.

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

Zhang, Rong published the artcileIodine-Catalyzed Construction of Dihydrooxepines via 3-Methyl-5-Pyrazolones C-H Oxidation/Functionalization of Quinolines Cascade, COA of Formula: C10H9ClN2O, the publication is European Journal of Organic Chemistry (2021), 2021(27), 3807-3811, database is CAplus.

An efficient iodine-catalyzed [3+3+1] annulation for the construction of dihydrooxepine scaffolds with quinoline units was developed. This strategy involved a seven-membered dihydrooxepine with a broad substrate scope through a formal three-component tandem reaction. Further derivation of the target product produced a trioxabicycle scaffold, which formed the basic core of natural products and pharmaceutical mols.

European Journal of Organic Chemistry 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 C9H9BrO2, COA of Formula: C10H9ClN2O.

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

Luo, Zhibo published the artcileDiscovery and optimization of selective RET inhibitors via scaffold hopping, Application of 2-Chloro-6-methyl-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128149, database is CAplus and MEDLINE.

Aberrant alterations of rearranged during transfection (RET) have been identified as actionable drivers of multiple cancers, including thyroid carcinoma and lung cancer. Currently, several approved multikinase inhibitors such as vandetanib and cabozantinib demonstrate clin. activity in patients with RET-rearranged or RET-mutant cancers. However, the observed response rates are only modest and the ‘off-target’ toxicities resulted from the inhibition of other kinases is also a concern. Herein, we designed and synthesized a series of RET inhibitors based on the structure of selective RET inhibitor BLU-667 and investigated their biol. activities. We identified compound I as a novel potent and selective RET inhibitor with improved drug-like properties. Compound I exhibits a selective inhibitory profile with an inhibitory concentration 50 (IC₅₀) of 1.29 nM for RET and 1.97 (RET V804M) or 0.99 (RET M918T) for mutant RETs. The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion was effectively suppressed by compound I (IC₅₀ = 19 nM). Addnl., compound 9 displayed less ‘off-target’ effects than BLU-667. In mouse xenograft models, compound I repressed tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner. Based on its exceptional kinase selectivity, good potency and high exposure in tumor tissues, compound 9 represents a promising lead for the discovery of RET directed therapeutic agents and the study of RET-driven tumor biol.

Bioorganic & Medicinal Chemistry Letters published new progress about 851435-28-4. 851435-28-4 belongs to pyrazoles-derivatives, auxiliary class Imidazole,Pyrimidine,Chloride,Amine, name is 2-Chloro-6-methyl-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine, and the molecular formula is C9H10ClN5, Application of 2-Chloro-6-methyl-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine.

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

Wu, Nan published the artcileSyntheses of pyrazole derivatives, Product Details of C10H9ClN2O, the publication is Daxue Huaxue (2014), 29(3), 63-66, database is CAplus.

Through the synthesis experiments of pyrazole derivatives, the students were led to use chem. open experiment time, search literatures, determine exptl. contents, complete experiment process and verify experiment results. A new rapid and simple method to synthesize pyrazole derivatives was found, and the creative consciousness and comprehensive abilities of students were improved.

Daxue Huaxue 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 C9H9ClO4, Product Details of C10H9ClN2O.

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

Maquestiau, A. published the artcileTautomerism in the pyrazolinone series. II. Solvent influence on the prototropic equilibrium of N1 substituted pyrazolin-5-ones, Related Products of pyrazoles-derivatives, the publication is Bulletin des Societes Chimiques Belges (1973), 82(3-4), 215-31, database is CAplus.

The solvent effect on the tautomerism of N-1 substituted pyrazolin-5-ones was determined by ir. The % keto form (I) was larger than the % enol form in nonpolar solvents; the % keto form decreased in aprotic solvents with their increasing basicity. In aprotic solvents, the concentration of the NH form (II) was related to the solvent acidity.

Bulletin des Societes Chimiques Belges 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, Related Products of pyrazoles-derivatives.

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

Simov, D. published the artcileAzo dye from 10-methyl-2-aminophenothiazine, Safety of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Godishnik na Sofiiskiya Universitet Sv. Kliment Okhridski, Khimicheski Fakultet (1975), 543-54, database is CAplus.

Azo dyes (I, R = pyrazolone, hydroxynaphthalene, aniline, aminonaphthalene residues) were prepared by coupling diazotized 2-amino-10-methylphenothiazine [2031-24-5] with RH and dyed protein and synthetic fibers wetfast and, in some cases, lightfast shades. All dyes were characterized by elementary anal., m.p., visible, uv, and ir spectra, and Rf. In I where R is not a pyrazolone residue the equilibrium between the azo enol form and the quinone hydrazone form is fully shifted to the azo enol form.

Godishnik na Sofiiskiya Universitet Sv. Kliment Okhridski, Khimicheski Fakultet 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 C8H17Br, Safety of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Padmaja, Pannala published the artcileSynthesis, molecular docking and in vitro antiproliferative activity of novel pyrano[3,2-c]carbazole derivatives, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is New Journal of Chemistry (2016), 40(10), 8305-8315, database is CAplus.

A new series of polycyclic pyrano[3,2-c]carbazole derivatives have been synthesized by domino Knoevenagel-hetero-Diels-Alder reactions. The key strategy involves ethylenediamine diacetate (EDDA) catalyzed cyclization of the O-prenyl derivative of N-Boc-carbazole-3-carboxaldehyde with cyclic 1,3-diketones or pyrazol-5-ones to afford cis-fused N-Boc-pyrano[3,2-c]carbazole derivatives The reactions were clean and highly diastereoselective, affording the desired products in good yields. The deprotection of the Boc group under acidic conditions led to pyrano[3,2-c]carbazole derivatives The antiproliferative activity of all the synthesized compounds on three cancer cell lines such as PANC 1 (pancreatic), HeLa (cervical) and MDA-MB-231 (breast cancer) was investigated. Three compounds including I displayed pronounced antiproliferative activity. The antimicrobial activity of these compounds was assayed against three representative Gram-pos. organisms and Gram-neg. organisms. Compound I exhibited significant antimicrobial activity. Mol. docking studies revealed that the lead compounds selectively occupy the colchicine binding site of tubulin.

New Journal of Chemistry 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, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Toonchue, Saowanee published the artcileMetal-free direct oxidative C-C bond coupling of pyrazolones and quinoxalinones, Product Details of C10H9ClN2O, the publication is Organic Chemistry Frontiers (2018), 5(12), 1928-1932, database is CAplus.

A highly efficient transition metal-free oxidative chemo- and regioselective C-C bond coupling of pyrazolones and quinoxalinones mediated by K₂S₂O₈ was described. This reaction was conveniently carried out under mild conditions which gave various hydroxy-pyrazolyl quinoxalinone products in moderate to excellent yields in a short reaction time.

Organic Chemistry Frontiers 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 C5H5NO3S, Product Details of C10H9ClN2O.

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

Yang, Xiaoqun published the artcileAsymmetric Synthesis of Structurally Sophisticated Spirocyclic Pyrano[2,3-c]pyrazole Derivatives Bearing a Chiral Quaternary Carbon Center, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Organic Letters (2022), 24(29), 5474-5479, database is CAplus and MEDLINE.

A carbene-catalyzed enantio- and diastereoselective [2 + 4] cycloaddition reaction is developed for quick and efficient access to structurally complex multicyclic pyrano[2,3-c]pyrazole mols. I (R = Me, Ph, 1-naphthyl, etc.; R¹ = H, Me, F; R² = H, Br, F; R³ = H, Me; R⁴ = Me, Bn, Ac, H; R⁵ = Me, Ph, 2-chlorophenyl). The reaction tolerates a broad scope of substrates bearing various substitution patterns, with the multicyclic pyrano[2,3-c]pyrazole products I afforded in generally good to excellent yields and optical purities. The chiral mols. obtained from this approach have found promising applications in the development of novel bactericides for plant protection.

Organic Letters 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 C5H8N2O, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Asghar, Soneela published the artcileCobalt-Catalyzed Suzuki Biaryl Coupling of Aryl Halides, Synthetic Route of 14580-22-4, the publication is Angewandte Chemie, International Edition (2017), 56(51), 16367-16370, database is CAplus and MEDLINE.

Readily accessed cobalt pre-catalysts with N-heterocyclic carbene ligands catalyze the Suzuki cross-coupling of aryl chlorides and bromides with alkyllithium-activated arylboronic pinacolate esters. Preliminary mechanistic studies indicate that the cobalt species is reduced to Co⁰ during the reaction.

Angewandte Chemie, International Edition 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, Synthetic Route of 14580-22-4.

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