pyrazoles-derivatives

Jismy, Badr published the artcileEfficient access to 3,5-disubstituted 7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidines involving S_NAr and Suzuki cross-coupling reactions, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Molecules (2020), 25(9), 2062, database is CAplus and MEDLINE.

An efficient and original synthesis of various 3,5-disubstituted 7-(trifluoromethyl)pyrazolo [1,5-a]pyrimidines was reported. A library of compounds diversely substituted in C-3 and C-5 positions was easily prepared from a common starting material, 3-bromo-7-(trifluoromethyl)pyrazolo[1,5-a] pyrimidin-5-one. In C-5 position, a S_NAr type reaction was achieved by first activating the C-O bond of the lactam function with PyBroP (Bromotripyrrolidinophosphonium hexafluorophosphate), followed by the addition of amine or thiol giving monosubstituted derivatives, whereas in C-3 position, arylation was performed via Suzuki-Miyaura cross-coupling using the com. available aromatic and heteroaromatic boronic acids. Moreover, trifluoromethylated analogs of potent Pim1 kinase inhibitors were designed following this concise synthetic methodol.

Molecules 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, Recommanded Product: 1H-Pyrazole-4-boronic acid.

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

Aravindakshan, Aghil Soorya published the artcileAnalysis of bio-active compounds present in the leaves and stem of Trichosanthes roxb. using GC-MS technique with respect to its anti-inflammatory action, Recommanded Product: 1-Methylpyrazole, the publication is International Journal of Pharmacy and Pharmaceutical Sciences (2021), 13(2), 7-13, database is CAplus.

Structural elucidation studies on Trichosanthes lobata Et acetate and methanol extracts of leaf and stem parts through Gas Chromatog.-Mass Spectrometry (GC-MS) technique with respect to anti-inflammatory potential. Extracts obtained with shade dried and powd. samples in successive solvent extraction using Et acetate and methanol by Soxhlet apparatus and subjected to GC-MS anal. and interpreted for its anti-inflammatory compounds The study revealed that the extraction solvent used was able to recover compound of classes such as organic acid esters and conjugated alkaloids in larger quantities than other classes of compounds and they varied with leaf and stem and also with the polarity of solvents used. In total compounds identified, GC-MS profile of the Et Acetate leaf extract of T. lobata contained 41 compounds, stem extract contained 45 compounds which have reported bioassays in PubChem. Whereas GC-MS profile of methanol leaf extract of T. lobata contained 66 compounds and stem extract contained 46 compounds having bioassay reports in PubChem. A large number of phytochem. peaks with good area percentage were found in methanolic extract We were also able to find out potent anti-inflammatory compounds including Octanoic acid, Dodecanoic acid, Octadecane, Enoic acid, Hexanoic acid, Quinazolin-8-one, Ilicic acid, Pentadecanoic acid, Oxaspiro, Benzeneacetic acid, etc. from the extracts T. lobata contains phytocompounds against inflammation which may serve as a new drug lead of natural products origin in future and make it employable in modern pharmacol. practices.

International Journal of Pharmacy and Pharmaceutical Sciences 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, Recommanded Product: 1-Methylpyrazole.

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

Gowri, M. published the artcileNovel Heterocyclic Schiff Base, (Z)-4-((2-((2-Aminophenyl)disulfanyl)phenylimino) (Phenyl)Methyl)-3-Methyl-1-Phenyl-1H-Pyrazol-5-ol Crystals for Enzymatic Studies, Name: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Molecular Crystals and Liquid Crystals (2015), 606(1), 199-207, database is CAplus.

A new dithio Schiff base was synthesized and characterized by spectroscopic (FTIR, UV-visible, H¹-NMR, and C¹³-NMR) and x-ray diffraction studies. Mol. interactions (inter and intra) between the neutral entities are discussed. Schiff base ligand, (Z)-4-((2-((2-aminophenyl)disulfanyl)phenylimino)(phenyl)methyl)-3-methyl-1-phenyl-1H-pyrazol-5-ol (), was synthesized by the reaction between 2-phenyl-4-benzoyl-5-methyl-pyrazolin-3-one and 2-amino thio phenol (1:2 molar ratio). The structural elucidation was done by spectroscopic (FTIR, UV-visible, H¹-NMR, C¹³-NMR) and x-ray diffraction studies. Single crystal x-ray diffraction studies revealed that has monoclinic system with space group P21/c with a 15.654(4) Å, b 12.848(4) Å, c 14.219(4) Å; α 90., β 113.65(6), γ 90.°, and Z = 4. The possible intramol. (C-H···N) and intermol. (C-H···O, C-H···S, N-H···O) interactions of were also been discussed.

Molecular Crystals and Liquid Crystals 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 C17H14N2O2, Name: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one.

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

Lee, Liang Wei published the artcileModulation of the volatile and non-volatile profiles of coffee fermented with Yarrowia lipolytica: II. Roasted coffee, Recommanded Product: 1-Methylpyrazole, the publication is LWT–Food Science and Technology (2017), 32-42, database is CAplus.

The fermentation of green coffee beans by Yarrowia lipolytica led to significant changes in the volatile and non-volatile profiles of green coffees (Part I). Therefore, the objective of this continuation study was to evaluate the effects of fermentation after roasting by characterizing the volatile profiles of coffees at three different roast levels and non-volatile profiles of coffee where the effects of fermentation on volatiles were most prominent (light roast). Y. lipolytica fermentation led to significant changes in the volatile profiles of roasted coffees which arose from both the modification of aroma precursors and the retention of volatile profile changes observed in green fermented coffees. The levels of 4-vinylguaiacol and 4-vinylphenol were 1.2-fold and 1.6-fold higher in light roasted fermented coffees resp. and could be explained by the higher levels detected in green fermented coffees before roasting. The levels of γ-butyrolactone were 5 times higher in light roasted fermented coffees than unfermented coffees. The increase in sulfur compounds levels and decrease in ketones levels were attributed to changes in the concentrations of aroma precursors like sugars and amino acids. Thus, this study highlighted the potential of utilizing yeast fermentation of green coffee beans for coffee aroma modulation.

LWT–Food Science and Technology 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, Recommanded Product: 1-Methylpyrazole.

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

Lim, Jongwon published the artcileDiscovery of 1-Amino-5H-pyrido[4,3-b]indol-4-carboxamide Inhibitors of Janus Kinase 2 (JAK2) for the Treatment of Myeloproliferative Disorders, Synthetic Route of 724710-02-5, the publication is Journal of Medicinal Chemistry (2011), 54(20), 7334-7349, database is CAplus and MEDLINE.

The JAK-STAT pathway mediates signaling by cytokines, which control survival, proliferation, and differentiation of a variety of cells. In recent years, a single point mutation (V617F) in the tyrosine kinase JAK2 was found to be present with a high incidence in myeloproliferative disorders (MPDs). This mutation led to hyperactivation of JAK2, cytokine-independent signaling, and subsequent activation of downstream signaling networks. The genetic, biol., and physiol. evidence suggests that JAK2 inhibitors could be effective in treating MPDs. De novo design efforts of new scaffolds identified 1-amino-5H-pyrido[4,3-b]indol-4-carboxamides as a new viable lead series. Subsequent optimization of cell potency, metabolic stability, and off-target activities of the leads led to the discovery of 7-(2-aminopyrimidin-5-yl)-1-{[(1R)-1-cyclopropyl-2,2,2-trifluoroethyl]amino}-5H-pyrido[4,3-b]indole-4-carboxamide (65). Compound 65 is a potent, orally active inhibitor of JAK2 with excellent selectivity, PK profile, and in vivo efficacy in animal models.

Journal of Medicinal Chemistry 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, Synthetic Route of 724710-02-5.

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

Cheng, Yuan-Zheng published the artcileSynthesis and crystal structure of Pb(II) complex with 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone, Recommanded Product: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Main Group Metal Chemistry (2014), 37(3-4), 101-106, database is CAplus.

A new Pb(II) complex, Pb(PMBP)₂ (PMBP = 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone), was synthesized and characterized by IR spectroscopy and x-ray single-crystal diffraction. X-ray crystallog. data showed that the complex crystallizes in the monoclinic space group C2 with a 22.060(7), b 6.981(2), c 9.127(3) Å, β = 90.768(7), C₃₄H₂₆N₄O₄Pb, Mr = 761.79, D = 1.800 g/cm³, μ(MoKa) = 6.050, F(000) = 744, Z = 2, final GooF = 1.067, R = 0.0195, and R_w = 0.0468 for 1353 observed reflections [I>2σ(I)]. The compound exhibits monomeric species that were linked by a C-H···π interaction, intermol. C-H···O H bonds, and intermol. longer secondary Pb···X (X = C or N) interactions; therefore, two-dimensional layered networks were obtained.

Main Group Metal Chemistry 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 C17H14N2O2, Recommanded Product: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one.

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

Guo, X. Q. published the artcileDual dispersive extraction combined with electrothermal vaporization inductively coupled plasma mass spectrometry for determination of trace REEs in water and sediment samples, Category: pyrazoles-derivatives, the publication is RSC Advances (2014), 4(38), 19960-19969, database is CAplus.

A simple and efficient two-step method based on dispersive solid phase extraction (D-SPE) and dispersive liquid-liquid microextraction (DLLME) was developed for the separation and preconcentration of 15 rare earth elements (REEs) from environmental water and sediment samples, followed by electrothermal vaporization-inductively coupled plasma mass spectrometry (ETV-ICP-MS) detection. With Chelex 100 as the adsorbent of D-SPE, target REEs were firstly extracted and the retained REEs were then desorbed by 0.1 mol L^-1 HNO₃. After 125 mmol L^-1 Tris and 40 mmol L^-1 1-phenyl-3-methyl-4-benzoylpyrazolone (PMBP) were added into the above elution solution, target REEs were further preconcd. into CCl₄ by DLLME. The developed dual extraction technique exhibited high enrichment factors (234 to 566-fold) and good anti-interference ability. Various parameters affecting the extraction of target REEs by D-SPE and DLLME were investigated in detail. Nder the optimal conditions, the limits of detection (LODs, 3σ) for target REEs were in the range of 0.003-0.073 ng L^-1 with the RSDs (C_{Y,La,Ce,Pr,Nd,Gd,Dy} = 1.0 ng L^-1, C_{Sm,Eu,Tb,Ho,Er,Tm,Yb,Lu} = 0.2 ng L^-1, n = 7) ranging from 6.7 to 11.5%. The proposed method of D-SPE-DLLME-ETV-ICP-MS was successfully applied to the determination of 15 REEs in water and sediment samples with the recoveries of 78-115% and 75-117% for the spiked water and sediment samples, resp. To validate the accuracy of the method, a Certified Reference Material of GBW07301a stream sediment was analyzed and the determined values were in good agreement with the certified values.

RSC Advances 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 C17H14N2O2, Category: pyrazoles-derivatives.

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

Li, Wenjing published the artcileStereodivergent Synthesis of Alkenylpyridines via Pd/Cu Catalyzed C-H Alkenylation of Pyridinium Salts with Alkynes, Recommanded Product: 1-Methylpyrazole, the publication is Organic Letters (2020), 22(20), 7814-7819, database is CAplus and MEDLINE.

The first Pd/Cu catalyzed selective C2-alkenylation of pyridines with internal alkynes has been developed via the pyridinium salt activation strategy. Importantly, the configuration of the product alkenylpyridines could be tuned by the choice of the proper N-alkyl group of the pyridinium salts, thus allowing for both the Z- and E-alkenylpyridines synthesized with good regio- and stereoselectivity. A plausible mechanism was proposed based on the Hammett study and KIE experiment

Organic Letters 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, Recommanded Product: 1-Methylpyrazole.

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

Lu, Xiaoyun published the artcileDiscovery of new chemical entities as potential leads against Mycobacterium tuberculosis, Product Details of C7H11N3O2, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(24), 5916-5919, database is CAplus and MEDLINE.

A series of biheterocyclic (1H-indole, benzofuran, pyrazolo[1,5-a]pyrimidine, pyrazolo[1,5-a]pyrimidin-5(4H)-one, imidazo[2,1-b]thiazole, and pyrazolo[5,1-b]thiazole) derivatives were synthesized and evaluated for their anti-tubercular activities. The imidazo[2,1-b]thiazoles and pyrazolo[5,1-b]thiazoles exhibited promising anti-tubercular activity in varying degrees. Especially, the 2,6-dimethylpyrazolo[5,1-b]thiazole exhibited strong suppressing function against H37Ra strain with MIC value of 0.03 μg/mL. This compound also displayed good pharmacokinetic profiles with oral bioavailability (F) of 41.7% and a half-life of 13.4 h. Furthermore, this compound significantly reduced the bacterial burden in an autoluminescent H37Ra infected mouse model, suggesting its promising potential for development of anti-tubercular drugs.

Bioorganic & Medicinal Chemistry Letters published new progress about 23286-70-6. 23286-70-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Ester, name is Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, and the molecular formula is C7H11N3O2, Product Details of C7H11N3O2.

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

Feng, Kai-Xiang published the artcileEnantioselective Syntheses of C₂-Symmetric Pyrazolones and Diones via One-Pot Organo-/Iodine Sequential Catalysis, Synthetic Route of 14580-22-4, the publication is Organic Letters (2021), 23(17), 6750-6755, database is CAplus and MEDLINE.

The catalytic diastereo- and enantioselective synthesis of C₂-sym. axially chiral 1,4-dicarbonyl derivatives with 2,3-quaternary stereocenters I (R = 3-bromophenyl, 2-methylphenyl, 3-chlorophenyl; R¹ = n-Pr, Ph, naphthalen-1-yl, thiophen-2-yl, etc.; R² = Et, Pr, i-Pr, cyclopropyl), II (R = i-Pr, 2-fluorophenyl, 2-nitrophenyl, etc.; R² = Ph, 4-fluorophenyl, 4-bromophenyl, etc.; R³ = Ph, naphthalen-2-yl, furan-2-yl, etc.) and III was achieved by utilizing an organo-/iodine binary catalytic strategy. The reactions proceeded well under mild conditions without metals or strong bases.

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 C10H9ClN2O, Synthetic Route of 14580-22-4.

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