Tag: 100-200

《A Facile and Solvent-Free Silica-Supported Route for the Preparation of Pyrazolium Salts and Its Catalytic Responses》 was published in Journal of Heterocyclic Chemistry in 2017. These research results belong to Ramalingam, Tamilarasan; Kilivelu, Ganesan. Application In Synthesis of Ethyl 5-amino-1-methyl-1H-pyrazole-3-carboxylate The article mentions the following:

Synthesis of di/trimeric substituted pyrazolium salts, e.g., I was carried out under a conventional/solvent-free silica-supported muffle furnace method. The solid phase method observed remarkable response compared with the conventional method for the preparation of pyrazolium salts. Di/trimeric substituted pyrazolium salts were acted as a very good catalyst for diaryl glycolic acid RC6H4C(OH)(COOH)(C6H4R) (R = H, 2-NO2, 3-MeO, 4-OH) preparation while compared with existing literatures. In addition to this study using Ethyl 5-amino-1-methyl-1H-pyrazole-3-carboxylate, there are many other studies that have used Ethyl 5-amino-1-methyl-1H-pyrazole-3-carboxylate(cas: 70500-80-0Application In Synthesis of Ethyl 5-amino-1-methyl-1H-pyrazole-3-carboxylate) was used in this study.

Ethyl 5-amino-1-methyl-1H-pyrazole-3-carboxylate(cas: 70500-80-0) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Application In Synthesis of Ethyl 5-amino-1-methyl-1H-pyrazole-3-carboxylate

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

In 2018,Moegling, Julian; Hoffmann, Alexander; Thomas, Fabian; Orth, Nicole; Liebhaeuser, Patricia; Herber, Ulrich; Rampmaier, Robert; Stanek, Julia; Fink, Gerhard; Ivanovic-Burmazovic, Ivana; Herres-Pawlis, Sonja published 《Designed To React: Terminal Copper Nitrenes and Their Application in Catalytic C-H Aminations》.Angewandte Chemie, International Edition published the findings.Electric Literature of C4H3F3N2 The information in the text is summarized as follows:

Heteroscorpionate ligands of the bis(pyrazolyl)methane family have been applied in the stabilization of terminal copper tosyl nitrenes. These species are highly active intermediates in the copper-catalyzed direct C-H amination and nitrene transfer. Novel perfluoroalkyl-pyrazolyl- and pyridinyl-containing ligands were synthesized to coordinate to a reactive copper nitrene center. Four distinct copper tosyl nitrenes were prepared at low temperatures by the reaction with SO2tBuPhINTs and copper(I) acetonitrile complexes. Their stoichiometric reactivity has been elucidated regarding the imination of phosphines and the aziridination of styrenes. The formation and thermal decay of the copper nitrenes were investigated by UV/Vis spectroscopy of the highly colored species. Addnl., the compounds were studied by cryo-UHR-ESI mass spectrometry and DFT calculations In addition, a mild catalytic procedure has been developed where the copper nitrene precursors enable the C-H amination of cyclohexane and toluene and the aziridination of styrenes. In the experimental materials used by the author, we found 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Electric Literature of C4H3F3N2)

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.Electric Literature of C4H3F3N2

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

In 2013,Selby, Thomas P.; Lahm, George P.; Stevenson, Thomas M.; Hughes, Kenneth A.; Cordova, Daniel; Annan, I. Billy; Barry, James D.; Benner, Eric A.; Currie, Martin J.; Pahutski, Thomas F. published 《Discovery of cyantraniliprole, a potent and selective anthranilic diamide ryanodine receptor activator with cross-spectrum insecticidal activity》.Bioorganic & Medicinal Chemistry Letters published the findings.Application of 20154-03-4 The information in the text is summarized as follows:

Anthranilic diamides are an exceptionally active class of insect control chem. that selectively activates insect ryanodine receptors causing mortality from uncontrolled release of calcium ion stores in muscle cells. Work in this area led to the successful commercialization of chlorantraniliprole for control of Lepidoptera and other insect pests at very low application rates. In search of lower log P analogs with improved plant systemic properties, exploration of cyano-substituted anthranilic diamides culminated in the discovery of a second product candidate, cyantraniliprole, having excellent activity against a wide range of pests from multiple insect orders. Here we report on the chem., biol. and structure-activity trends for a series of cyanoanthranilic diamides from which cyantraniliprole was selected for com. development. In the experiment, the researchers used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application of 20154-03-4)

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.Application of 20154-03-4

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

In 2012,Smith, Garry R.; Caglic, Dejan; Capek, Petr; Zhang, Yan; Godbole, Sujata; Reitz, Allen B.; Dickerson, Tobin J. published 《Reexamining hydroxamate inhibitors of botulinum neurotoxin serotype A: Extending towards the β-exosite》.Bioorganic & Medicinal Chemistry Letters published the findings.Application In Synthesis of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:

Botulinum neurotoxins (BoNTs) are the most toxic proteins known to man, exposure to which results in flaccid paralysis. Given their extreme potency, these proteins have become studied as possible weapons of bioterrorism; however, effective treatments that function after intoxication have not progressed to the clinic. Here, we have reexamined one of the most effective inhibitors, 2,4-dichlorocinnamyl hydroxamate, in the context of the known plasticity of the BoNT/A light chain metalloprotease. Our studies have shown that modifications of this compound are tolerated and result in improved inhibitors, with the best compound having an IC50 of 0.23 μM. Given the inconsistency of structure-activity relationship trends observed across similar compounds, this data argues for caution in extrapolating across structural series. In addition to this study using 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, there are many other studies that have used 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Application In Synthesis of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole) was used in this study.

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Application In Synthesis of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

In 2019,Angewandte Chemie, International Edition included an article by Nemec, Vaclav; Hylsova, Michaela; Maier, Lukas; Flegel, Jana; Sievers, Sonja; Ziegler, Slava; Schroeder, Martin; Berger, Benedict-Tilman; Chaikuad, Apirat; Valcikova, Barbora; Uldrijan, Stjepan; Drapela, Stanislav; Soucek, Karel; Waldmann, Herbert; Knapp, Stefan; Paruch, Kamil. Application In Synthesis of Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate. The article was titled 《Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway》. The information in the text is summarized as follows:

Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic sequences based on chemoselective metal-mediated couplings, including assembly of the furo[3,2-b]pyridine scaffold by copper-mediated oxidative cyclization. Optimization of the subseries containing 3,5-disubstituted furo[3,2-b]pyridines, e.g. I, afforded potent, cell-active, and highly selective inhibitors of CLKs. Profiling of the kinase-inactive subset of 3,5,7-trisubstituted furo[3,2-b]pyridines, e.g. II, revealed sub-micromolar modulators of the Hedgehog pathway. The experimental process involved the reaction of Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate(cas: 1258323-45-3Application In Synthesis of Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate)

Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate(cas: 1258323-45-3) 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. Application In Synthesis of Potassium trifluoro(1-methyl-1H-pyrazol-5-yl)borate

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

Recommanded Product: Methyl 1H-pyrazole-3-carboxylateIn 1991 ,《Effect of electron-withdrawing groups on the thermal ring opening of 3H-pyrazoles to diazoalkenes》 was published in Journal of Chemical Research, Synopses. The article was written by Nakano, Yoshihiko; Hamaguchi, Masashi; Nagai, Toshikazu. The article contains the following contents:

3-Cyano-3H-pyrazoles, bearing a cyano, a p-chlorophenyl, or a p-chlorobenzyl group at C-3, e.g. I, generated from elimination reaction of the corresponding dihydropyrazoles with a leaving group such as a chlorine or p-chlorobenzoyloxy group, gave diazoalkene derivatives, resulting from the ring-opening of the 3H-pyrazoles. 3-Methoxycarbonyl-3H-pyrazoles bearing a methoxycarbonyl, a p-chlorophenyl, or p-chlorobenzyl group at C-3, prepared in a similar manner, gave mainly 1-methoxycarbonyl-1H-pyrazole derivatives, resulting from migration of the 3-methoxycarbonyl group to the adjacent nitrogen within the generated 3H-pyrazoles. Treatment of 3H-pyrazoles and 5-substituted 1-methoxycarbonyl-1H-pyrazoles with triethylamine gave 3-substituted 1-methoxycarbonyl-1H-pyrazoles, resulting from migration of the methoxycarbonyl group to the remote nitrogen. The experimental part of the paper was very detailed, including the reaction process of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Recommanded Product: Methyl 1H-pyrazole-3-carboxylate)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) 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: Methyl 1H-pyrazole-3-carboxylate

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

Name: 3-(Trifluoromethyl)-1H-pyrazoleIn 2015 ,《Synthesis, characterization, and ethylene polymerization behavior of Cr(III) catalysts based on bis(pyrazolylmethyl)pyridine and its derivatives》 appeared in Journal of Molecular Catalysis A: Chemical. The author of the article were Woo, Jeong Oh; Kang, Sung Kwon; Park, Jong-Eun; Son, Kyung-sun. The article conveys some information:

New chromium(III) [Cr(III)] catalysts based on 2,6-bis(1-pyrazolylmethyl)pyridine derivatives have been synthesized, characterized, and evaluated for ethylene polymerization All ligands with substituents on the pyrazole rings were analyzed by single-crystal X-ray diffraction to clearly identify isomer structures. Addnl., X-ray analyses of a new Cr(III) complex bearing 2,6-bis[(4,5-dimethyl-1H-pyrazol-1-yl)methyl]pyridine showed tridentate coordination on the mer-octahedral chromium sphere. Upon activation with dry Me aluminoxane, the precatalysts produce polyethylene (PE) as a major product, and their catalytic performances were affected by the substituents on the pyrazole units; the introduction of functional groups on the pyrazole compositions and the mol. weight of the PE. 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. 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.Name: 3-(Trifluoromethyl)-1H-pyrazole

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

COA of Formula: C4H3F3N2In 2010 ,《Pyrazole synthesis under microwave irradiation and solvent-free conditions》 appeared in Journal of the Brazilian Chemical Society. The author of the article were Buriol, Lilian; Frizzo, Clarissa P.; Marzari, Mara R. B.; Moreira, Dayse N.; Prola, Lizie D. T.; Zanatta, Nilo; Bonacorso, Helio G.; Martins, Marcos A. P.. The article conveys some information:

Solvent-free reaction conditions using microwave irradiation (MW) were studied in preparation of 4,5-dihydro-1H-pyrazoles and dehydrated pyrazoles by the cyclocondensation reaction of 4-alkoxy-1,1,1-trifluoro-3-alken-2-ones [CF3C(O)CH=C(R1)OR, where R/R1 = Et/H, Me/Me and Me/Ph] with hydrazines [NH2NH-R2, where R2 = CO2Me, Ph, CH2CH2OH]. Some reactions were performed under the same reaction conditions using methanol as solvent. The results obtained using MW equipment for synthesis under solvent-free conditions were also compared with those described in literature for conventional thermal heating and heating with a domestic MW oven. In general, the products furnished by reaction in MW equipment for synthesis presented better yields and shorter reaction times. In addition, it was demonstrated that the reaction temperature altered the formation of products for each hydrazine showing that MW equipment for synthesis is efficient for reacting hydrazines and 4-alkoxy-1,1,1-trifluoro-3-alken-2-ones to procedure the products 4,5-dihydro-1H-pyrazoles and dehydrated pyrazoles. The experimental part of the paper was very detailed, including the reaction process of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4COA of Formula: C4H3F3N2)

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.COA of Formula: C4H3F3N2

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

Electric Literature of C4H3F3N2In 2010 ,《A novel series of positive modulators of the AMPA receptor: Discovery and structure based hit-to-lead studies》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Jamieson, Craig; Basten, Stephanie; Campbell, Robert A.; Cumming, Iain A.; Gillen, Kevin J.; Gillespie, Jonathan; Kazemier, Bert; Kiczun, Michael; Lamont, Yvonne; Lyons, Amanda J.; MacLean, John K. F.; Moir, Elizabeth M.; Morrow, John A.; Papakosta, Marianthi; Rankovic, Zoran; Smith, Lynn. The article conveys some information:

Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22 (I), a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor. In the part of experimental materials, we found many familiar compounds, such as 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Electric Literature of C4H3F3N2)

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.Electric Literature of C4H3F3N2

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

《Bridge-Clamp Bis(tetrazine)s with [N]8 π-Stacking Interactions and Azido-s-Aryl Tetrazines: Two Classes of Doubly Clickable Tetrazines》 was published in Angewandte Chemie, International Edition in 2020. These research results belong to Mboyi, Cleve D.; Vivier, Delphine; Daher, Ahmad; Fleurat-Lessard, Paul; Cattey, Helene; Devillers, Charles H.; Bernhard, Claire; Denat, Franck; Roger, Julien; Hierso, Jean-Cyrille. Application of 20154-03-4 The article mentions the following:

Click chem. at a tetrazine core is useful for bioorthogonal labeling and crosslinking. Introduced here are two new classes of doubly clickable s-aryl tetrazines synthesized by Cu-catalyzed cross-coupling. Homocoupling of o-brominated s-aryl tetrazines leads to bis(tetrazine)s structurally characterized by tetrazine cores arranged face-to-face. [N]8 π-stacking interactions are essential to the conformation. Upon inverse electron demand Diels-Alder (iEDDA) cycloaddition, the bis(tetrazine)s produce a unique staple structure. The o-azidation of s-aryl tetrazines introduces a second proximal intermol. clickable function that leads to double click chem. opportunities. The stepwise introduction of fluorophores and then iEDDA cycloaddition, including bioconjugation to antibodies, was achieved on this class of tetrazines. This method extends to (thio)etherification, phosphination, trifluoromethylation and the introduction of various bioactive nitrogen-based heterocycles. The experimental part of the paper was very detailed, including the reaction process of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application of 20154-03-4)

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.Application of 20154-03-4

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