Month: November 2022

Peng, Yingyuan published the artcilePd-Catalyzed intramolecular C-H activation and C-S formation to synthesize pyrazolo[5,1-b]benzothiazoles without an additional oxidant, SDS of cas: 14580-22-4, the publication is Organic Chemistry Frontiers (2019), 6(18), 3234-3237, database is CAplus.

An efficient synthesis of pyrazolo[5,1-b]benzothiazole scaffold via Pd-catalyzed intramol. C-H activation and C-S formation was reported. By starting from easily available 1-phenyl-1H-pyrazole-5-thiol compounds, a series of substituted pyrazolo[5,1-b]benzothiazoles were obtained with moderate to good yields. Interestingly, this reaction didn’t need any addnl. oxidant and the reaction conditions were also suitable for the synthesis of imidazo[2,1-b]benzothiazole derivatives

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 C10H9ClN2O, SDS of cas: 14580-22-4.

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

Wang, Yuting published the artcileDesign, synthesis, and biological evaluation of pyrano[2,3-c]pyrazole-Based RalA inhibitors against hepatocellular carcinoma, Computed Properties of 14580-22-4, the publication is Frontiers in Chemistry (Lausanne, Switzerland) (2021), 700956, database is CAplus and MEDLINE.

The discovery of a series of 6-sulfonylamide-pyrano[2,3-c]pyrazole derivatives I [R = H, 4-Me, 2-MeO, etc.; R¹ = C₆H₅, 4-MeC₆H₄, 4-MeOC₆H₄, etc.; R² = C₆H₅, 4-MeC₆H₄, 3-MeOC₆H₄, etc.] as novel RalA inhibitors was reported. ELISA-based biochem. assay results indicated that compounds I [R = H; R¹ = 4-MeC₆H₄, 4-MeOC₆H₄, 4-F₃CC₆H₄, 2,4-di-FC₆H₃, 2-thienyl; R² = 4-F₃CC₆H₄, 3-pyridyl, 4-pyridyl, 3-thienyl] suppressed RalA/B binding capacities to their substrates. Cellular proliferation assays indicated that these RalA inhibitors potently inhibited the proliferation of HCC cell lines, including HepG2, SMMC-7721, Hep3B, and Huh-7 cells. Among the evaluated compounds, compound I [R = H, R¹ = 4-MeOC₆H₄, R² = 4-F₃CC₆H₄] displayed good inhibitory capacities on RalA (IC₅₀ = 0.22渭M) and HepG2 cells (IC₅₀ = 2.28渭M). Overall, the results suggested that a novel small mol. RalA inhibitor with a 6-sulfonylamide-pyrano[2,3-c]-pyrazole scaffold suppressed autophagy and cell proliferation in hepatocellular carcinoma, and that it has potential for HCC-targeted therapy.

Frontiers in Chemistry (Lausanne, Switzerland) 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 C3H6O2, Computed Properties of 14580-22-4.

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

Lin, Jiao-Min published the artcileA Metal-Organic Framework with a Pore Size/Shape Suitable for Strong Binding and Close Packing of Methane, Formula: C8H7N3, the publication is Angewandte Chemie, International Edition (2016), 55(15), 4674-4678, database is CAplus and MEDLINE.

Much effort has been devoted to develop new porous structures for methane storage. We report a new porous coordination framework showing exceptional methane uptakes (e.g. 263 volume/volume at 298 K and 65 bar) and adsorption enthalpies (21.6 kJ mol^-1) as high as current record holders functionalized by open metal sites. Computational simulations demonstrated that the hierarchical pore structure consisting of single-wall nanocages has suitable sizes/shapes and organic binding sites to enforce not only strong host-methane and methane-methane interactions but also dense packing of methane mols.

Angewandte Chemie, International Edition published new progress about 19959-71-8. 19959-71-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Pyridine, name is 4-(1H-Pyrazol-4-yl)pyridine, and the molecular formula is C8H7N3, Formula: C8H7N3.

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

Lin, Jiao-Min published the artcileA novel pillared-layer-type porous coordination polymer featuring three-dimensional pore system and high methane storage capacity, Application In Synthesis of 19959-71-8, the publication is Science China: Chemistry (2016), 59(8), 970-974, database is CAplus.

Solvothermal reaction of Zn(NO₃)₂, 4-(1H-pyrazol-4-yl)pyridine (Hpypz) and 1,3,5-benzenetricarboxylic acid (H₃btc) in N,N-dimethylacetamide (DMA) produced a new porous coordination polymer [Zn₅(pypz)₄(btc)₂] (1). Single-crystal x-ray diffraction study of 1 showed that deprotonated pypz^– ligands served as 1,2,4-triazolate-like ligands, linking Zn(II) ions to form porous 2D sql-a layers {Zn(pypz)}⁺, which were further connected by eight-legged pillars {Zn₂(btc)₄(H₂O)₂}^8- based on the typical paddlewheel dinuclear Zn₂(RCOO)₄(H₂O)₂ cluster to form a novel type of noninterpenetrated pillared-layer framework with 3D intersecting pore system and large pore volume Gas sorption measurements revealed that 1 possesses a large BET surface area of 2061 m² g^-1 and very high methane total uptake of 245 cm³(STP) cm^-3 at 298 K and 65 bar.

Science China: Chemistry published new progress about 19959-71-8. 19959-71-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Pyridine, name is 4-(1H-Pyrazol-4-yl)pyridine, and the molecular formula is C8H7N3, Application In Synthesis of 19959-71-8.

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

Wang, Yu published the artcilePreparation of trace single oxidation state plutonium solutions, Product Details of C17H14N2O2, the publication is He Huaxue Yu Fangshe Huaxue (2014), 36(4), 200-204, database is CAplus.

The trace levels of single oxidation state plutonium (Pu(IV,V,VI)) solution was prepared, and the stability was monitored over time. The oxidation state distribution of the solution was analyzed by solvent extraction methods, in which Pu (IV) was extracted with TTA and Pu (IV + VI) was separated by HDEHP. The Pu (IV) solution is prepared by heating the solution until dryness in 1 mol/L HNO₃ repeatedly, and Pu (VI) solution is obtained by keeping Pu (IV) in 0.5-1 mol/L HNO₃-0.1 mmol/L KMnO₄ system for 24 h. Pu (1M) is reduced automatically to Pu (V) in the dark for 5 d. All of these single plutonium solutions could not keep steady in PH = 3.0, 0.01 mol/L NaCl system. Consequently, single oxidation state plutonium solutions need to be prepared freshly for each experiment

He Huaxue Yu Fangshe Huaxue 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 C6H8O3, Product Details of C17H14N2O2.

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

Gao, Qingqing published the artcilePalladium-catalyzed polyannulation of pyrazoles and diynes toward multifunctional poly(indazole)s under monomer non-stoichiometric conditions, Application In Synthesis of 930-36-9, the publication is Polymer Chemistry (2019), 10(39), 5296-5303, database is CAplus.

A new synthetic route toward multifunctional poly(indazole)s (PIs) with an effect of monomer stoichiometry imbalance-promoted polymerization is described in this work. The palladium-catalyzed oxidative polyannulations of internal diynes and 1-methylpyrazole proceed smoothly in 1,4-dioxane at 120掳C with copper acetate monohydrate functioning as the oxidant. A series of PIs with high mol. weights (M_w up to 35 800) are generated in good yields (up to 84.0%) under monomer non-stoichiometric conditions. These polymers exhibit high thermal stability, losing merely 5% of their weights at high temperatures of 321-353掳C. The solid thin films of these PIs show high and UV-tunable refractive indexes (n = 1.8870-1.6051) in a wide wavelength range of 400-900 nm. The tetraphenylethene-containing PI shows obvious solid-state emission properties and good photosensitivity. Its thin film was successfully fabricated into a well-defined two-dimensional fluorescent photopattern with sharp edges.

Polymer Chemistry 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, Application In Synthesis of 930-36-9.

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

Ryu, Jae Wook published the artcileDesign and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors, Synthetic Route of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(23), 7185-7188, database is CAplus and MEDLINE.

A series of triazolopyridazines substituted with methylisoquinolinone, e.g. I (R = Ph, pyrrolidin-1-yl, thiazol-3-yl, 3-FC₆H₄), were designed and synthesized. Some of the triazolopyridazines strongly inhibited c-Met kinase and showed good anti-proliferative activity against a panel of c-Met-amplified gastric cancer cell lines (MKN-45, SNU-5 and Hs746T).

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, Synthetic Route of 763120-58-7.

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

Ryu, Jae Wook published the artcileDesign and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors, Recommanded Product: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(23), 7185-7188, database is CAplus and MEDLINE.

A series of triazolopyridazines substituted with methylisoquinolinone, e.g. I (R = Ph, pyrrolidin-1-yl, thiazol-3-yl, 3-FC₆H₄), were designed and synthesized. Some of the triazolopyridazines strongly inhibited c-Met kinase and showed good anti-proliferative activity against a panel of c-Met-amplified gastric cancer cell lines (MKN-45, SNU-5 and Hs746T).

Bioorganic & Medicinal Chemistry Letters published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, Recommanded Product: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid.

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

Qian, Yimin published the artcileDiscovery of Highly Selective and Orally Active Lysophosphatidic Acid Receptor-1 Antagonists with Potent Activity on Human Lung Fibroblasts, Related Products of pyrazoles-derivatives, the publication is Journal of Medicinal Chemistry (2012), 55(17), 7920-7939, database is CAplus and MEDLINE.

Lysophosphatidic acid is a class of bioactive phospholipid that mediates most of its biol. effects through LPA receptors, of which six isoforms have been identified. The recent results from LPA1 knockout mice suggested that blocking LPA1 signaling could provide a potential novel approach for the treatment of idiopathic pulmonary fibrosis. Here, we report the design and synthesis of pyrazole- and triazole-derived carbamates as LPA1-selective and LPA1/3 dual antagonists. In particular, compound I, the most selective LPA1 antagonist reported, inhibited proliferation and contraction of normal human lung fibroblasts (NHLF) following LPA stimulation. Oral dosing of compound I to mice resulted in a dose-dependent reduction of plasma histamine levels in a murine LPA challenge model. Furthermore, we applied our novel antagonists as chem. probes and investigated the contribution of LPA1/2/3 in mediating the pro-fibrotic responses. Our results suggest LPA1 as the major receptor subtype mediating LPA-induced proliferation and contraction of NHLF.

Journal of Medicinal Chemistry published new progress about 105675-85-2. 105675-85-2 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Bromide,Amine, name is 4-Bromo-1-methyl-1H-pyrazol-5-amine, and the molecular formula is C4H6BrN3, Related Products of pyrazoles-derivatives.

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