Month: October 2022

《Structure-antitumor activity relationship of hybrid acetogenins focusing on connecting groups between heterocycles and the linker moiety》 was published in RSC Advances in 2022. These research results belong to Ohta, Kaito; Fushimi, Tetsuya; Okamura, Mutsumi; Akatsuka, Akinobu; Dan, Shingo; Iwasaki, Hiroki; Yamashita, Masayuki; Kojima, Naoto. Electric Literature of C4H6N2 The article mentions the following:

We studied hybrid mols. of annonaceous acetogenins and mitochondrial complex I-inhibiting insecticides to develop a novel anticancer agent. A structure-antitumor activity relationship study focusing on the connecting groups between the heterocycles and the linker moiety bearing the THF moiety was conducted. Eleven hybrid acetogenins with 1-methylpyrazole instead of γ-lactone were synthesized and their growth inhibitory activities against 39 human cancer cell lines were evaluated. The nitrogen atom at the 2′-position of the linker moiety was essential for inhibiting cancer growth. The 1-methylpyrazole-5-sulfonamide analog showed potent growth inhibition of NCI-H23, a human lung cancer cell line, in a xenograft mouse assay without critical toxicity. Hence, the results of this study may pave the way for the development of novel anticancer agents, with both selective and broad anticancer activities. In the experiment, the researchers used 1-Methylpyrazole(cas: 930-36-9Electric Literature of C4H6N2)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Electric Literature of C4H6N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Li, Guangbin; Field, James A.; Zeng, Chao; Madeira, Camila Leite; Nguyen, Chi Huynh; Jog, Kalyani Vikas; Speed, David; Sierra-Alvarez, Reyes published their research in Chemosphere on February 29 ,2020. The article was titled 《Diazole and triazole inhibition of nitrification process in return activated sludge》.Category: pyrazoles-derivatives The article contains the following contents:

Azoles are emerging contaminants that are resistant to biodegradation during wastewater treatment. Their presence has been widely reported in wastewater effluents and receiving waters. In this work, the potential inhibition of nitrification process by six different azole compounds in wastewater treatment plants was investigated in batch bioassays. The azoles studied included three diazoles: pyrazole (Pz); 1-methylpyrazole (MePz); 3,5-dimethylpyrazole (DMePz); and three triazoles: 1,2,4-triazole (Tz); benzotriazole (BTz); and 5-Me benzotriazole (MeBTz). The concentration of azoles causing 50% inhibition (IC50) increased (azoles became less inhibitory) in the following order (mg L-1): BTz (1.99) < MeBTz (2.18) < Pz (2.69) < Tz (3.53) < DMePz (17.3) < MePz (49.6). No clear structure-inhibitory relationships were found using Log P and pKa as structural properties. The toxicity of any given azole may be related to the role of substituent groups on disabling/enabling binding to the active sites of metallo-enzymes in nitrifying microorganisms. This is exemplified by the low toxicity of MePz, which has a cyclic N blocked by a Me group. The observed inhibition caused to nitrifying bacteria is more severe than their cytotoxicity to other target organisms (e.g., methanogens and heterotrophic bacteria), suggesting a specific inhibition to the copper-containing enzyme, ammonium monooxygenase, in ammonia oxidizing nitrifying microorganisms. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpyrazole(cas: 930-36-9Category: pyrazoles-derivatives)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Category: pyrazoles-derivatives

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

《Highly active hybrid mesoporous silica-supported base organocatalysts for C-C bond formation》 was written by Erigoni, A.; Hernandez-Soto, M. C.; Rey, F.; Segarra, C.; Diaz, U.. Recommanded Product: 930-36-9 And the article was included in Catalysis Today on April 1 ,2020. The article conveys some information:

New base hybrid catalysts, based on silyl-derivatives of mols. carrying amino, diamino, pyrrolidine, pyrazolium and imidazolium functionalities were successfully achieved through post synthetic grafting onto M41S-type support. Different characterization techniques were implemented to study the characteristics of the materials, such as elemental anal., solid state MAS NMR and FTIR spectroscopies, X-ray diffraction (XRD), thermogravimetric and differential thermal analyses (TGA-DTA) and textural properties through N2 physisorption anal. The catalytic activity and recyclability of these compounds as base catalysts was demonstrated for C-C bond forming reactions such as Knoevenagel condensations and Michael additions rationalizing the differences observed as function of the reaction mechanisms. An enamine mechanism was proposed for Knoevenagel condensations and an enolate mechanism for Michael additions The experimental process involved the reaction of 1-Methylpyrazole(cas: 930-36-9Recommanded Product: 930-36-9)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Recommanded Product: 930-36-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Category: pyrazoles-derivativesOn October 16, 2020 ,《Stereodivergent Synthesis of Alkenylpyridines via Pd/Cu Catalyzed C-H Alkenylation of Pyridinium Salts with Alkynes》 was published in Organic Letters. The article was written by Li, Wenjing; Tang, Juan; Li, Shun; Zheng, Xueli; Yuan, Maolin; Xu, Bin; Jiang, Weidong; Haiyan Fu; Li, Ruixiang; Chen, Hua. The article contains the following contents:

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 In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Category: pyrazoles-derivatives) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Category: pyrazoles-derivatives

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Britton, Luke; Skrodzki, Maciej; Nichol, Gary S.; Dominey, Andrew P.; Pawluc, Piotr; Docherty, Jamie H.; Thomas, Stephen P. published an article in ACS Catalysis. The title of the article was 《Manganese-Catalyzed C(sp2)-H Borylation of Furan and Thiophene Derivatives》.Quality Control of 1-Methylpyrazole The author mentioned the following in the article:

Aryl boronic esters are bench-stable, platform building-blocks that can be accessed through metal-catalyzed aryl C(sp2)-H borylation reactions. C(sp2)-H bond functionalization reactions using rare- and precious-metal catalysts are well established, and while examples using Earth-abundant alternatives have emerged, Mn catalysis remains lacking. The Mn-catalyzed C-H borylation of furan and thiophene derivatives is reported alongside an in situ activation method providing facile access to the active Mn hydride species. Mechanistic studies showed that blue light irradiation directly affected catalysis by action at the metal center, that C(sp2)-H bond borylation occurs through a C-H metalation pathway, and that the reversible coordination of pinacolborane to the catalyst gave a Mn borohydride complex, which was as an off-cycle resting state. The results came from multiple reactions, including the reaction of 1-Methylpyrazole(cas: 930-36-9Quality Control of 1-Methylpyrazole)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Quality Control of 1-Methylpyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2014,Seo, Samuel; Simoni, Luke D.; Ma, Mengting; DeSilva, M. Aruni; Huang, Yong; Stadtherr, Mark A.; Brennecke, Joan F. published 《Phase-Change Ionic Liquids for Postcombustion CO2 Capture》.Energy & Fuels published the findings.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

Phase-change ionic liquids, or PCILs, are salts that are solids at normal flue gas processing temperatures (e.g., 40-80°) and that react stoichiometrically and reversibly with CO2 (one mole of CO2 for every mole of salt at typical postcombustion flue gas conditions) to form a liquid Thus, the m.p. of the PCIL-CO2 complex is below that of the pure PCIL. A new concept for CO2 separation technol. that uses this key property of PCILs offers the potential to significantly reduce parasitic energy losses incurred from postcombustion CO2 capture by using the heat of fusion (ΔHfus) to provide part of the heat needed to release CO2 from the absorbent. The phase transition yields almost a step-change absorption isotherm, so only a small pressure or temperature swing is required between the absorber and the stripper. Using aprotic heterocyclic anions (AHAs), the enthalpy of reaction with CO2 can be readily tuned, and the phys. properties, such as m.p., can be adjusted by modifying the alkyl chain length of the tetra-alkylphosphonium cation. Here, the authors present data for 4 tetrabutylphosphonium salts that exhibit PCIL behavior, as well as detailed measurements of the CO2 solubility, phys. properties, phase transition behavior, and H2O uptake for tetraethylphosphonium benzimidazolide ([P2222][BnIm]). The process based on [P2222][BnIm] has the potential to reduce the amount of energy required for the CO2 capture process substantially compared to the current technol. that employs aqueous monoethanolamine (MEA) solvents. The experimental part of the paper was very detailed, including the reaction process of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

《Efficient copper-catalyzed cross-coupling of nitrogen nucleophiles with N,N-dibenzyl-4-iodobenzenesulfonamide and its application in the synthesis of Celecoxib intermediate》 was written by Yong, Fui-Fong; Azri, Miskal; Darrell Lim, Yong-En; Teo, Yong-Chua. Product Details of 20154-03-4 And the article was included in Tetrahedron in 2020. The article conveys some information:

A practical and efficient strategy has been developed for the cross-coupling of N,N-dibenzyl-4-iodobenzenesulfonamide with nitrogen nucleophiles using 0.5-20 mol% of CuI under ligand-free conditions. A variety of nitrogen nucleophiles including nitrogen heterocycles, sulfonamides and amides afforded the corresponding products in moderate to good yields (up to 98%) under the optimized conditions. The application of this catalytic system to the synthesis of Celecoxib intermediate was also successfully demonstrated. In addition to this study using 3-(Trifluoromethyl)-1H-pyrazole, there are many other studies that have used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Product Details of 20154-03-4) was used in this study.

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Product Details of 20154-03-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Shi, Jiale; Yuan, Tao; Wang, Rong; Zheng, Meifang; Wang, Xinchen published their research in Green Chemistry in 2021. The article was titled 《Boron carbonitride photocatalysts for direct decarboxylation: the construction of C(sp3)-N or C(sp3)-C(sp2) bonds with visible light》.COA of Formula: C5H6N2O2 The article contains the following contents:

A metal-free protocol was established for the decarboxylative N-H or C(sp2)-H functionalization of acids via metal-free boron carbon nitride (BCN) photocatalysis, delivering the desired products under ambient conditions. This methodol.was applicable to the late-stage modification of pharmaceutical mols. and gram-scale experiments as well as in the recovery and reuse of the photocatalysts without the loss of reactivity. The developed photochem. reaction system fulfills the requirements of green and sustainable chem. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4COA of Formula: C5H6N2O2)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.COA of Formula: C5H6N2O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2015,Nicolaou, K. C.; Rhoades, Derek; Wang, Yanping; Totokotsopoulos, Sotirios; Bai, Ruoli; Hamel, Ernest published 《Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues》.ChemMedChem published the findings.Name: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

The design, synthesis, and biol. evaluation of a series of epothilone analogs with novel side chains equipped with an amino group are described. Their design facilitates potential conjugation to selective drug delivery systems such as antibodies. Their synthesis proceeded efficiently via Stille coupling of a readily available vinyl iodide and heterocyclic stannanes. Cytotoxicity studies and tubulin binding assays revealed two of these analogs, I (R = CF3, F), to be more potent than epothilones A-D and the anticancer agent ixabepilone, currently in clin. use. The experimental process involved the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Name: 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Name: 3-(Trifluoromethyl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

The author of 《Palladium-Promoted DNA-Compatible Heck Reaction》 were Wang, Xuan; Sun, Hui; Liu, Jiaxiang; Zhong, Wenge; Zhang, Mingqiang; Zhou, Hu; Dai, Dongcheng; Lu, Xiaojie. And the article was published in Organic Letters in 2019. HPLC of Formula: 847818-74-0 The author mentioned the following in the article:

Optimal conditions for palladium-promoted Heck reaction on DNA were developed with good to excellent conversions. Versatility with either DNA-conjugated styrene/acrylamide or aryl iodide and a broad substrate scope of the corresponding coupling partners were established. Furthermore, robustness of the Heck reaction conditions on single-strand DNA and feasibility for DNA-encoded library production were demonstrated. After reading the article, we found that the author used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0HPLC of Formula: 847818-74-0)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. HPLC of Formula: 847818-74-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics