Month: October 2022

In 2016,Zhang, Jin; Jia, Run-Ping; Wang, Dong-Hui published 《Copper-catalyzed C-N cross-coupling of arylboronic acids with N-acylpyrazoles》.Tetrahedron Letters published the findings.Category: pyrazoles-derivatives The information in the text is summarized as follows:

A copper-catalyzed C-N bond forming reaction of arylboronic acids and N-acylpyrazoles was developed. This procedure used N-acetyl protected pyrazoles as starting material instead of free pyrazoles (NH). The reaction worked under neutral conditions and did not require any base or ligand. The reaction showed good functional group tolerance. In addition to this study using 3-(Trifluoromethyl)-1H-pyrazole, there are many other studies that have used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Category: pyrazoles-derivatives) was used in this study.

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.Category: pyrazoles-derivatives

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

Tanwar, Lalita; Boergel, Jonas; Lehmann, Johannes; Ritter, Tobias published their research in Organic Letters in 2021. The article was titled 《Selective C-H Iodination of (Hetero)arenes》.SDS of cas: 15366-34-4 The article contains the following contents:

A strategy for selective C-H iodination of (hetero)arenes was decribed with a broad functional group tolerance. The utility and differentiation to other iodination methods of supposed sulfonyl hypoiodites for a set of carboarenes and heteroarenes was described.Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4SDS of cas: 15366-34-4) was used in this study.

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.SDS of cas: 15366-34-4

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

Recommanded Product: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2017 ,《Stereoselective Photoredox-Catalyzed Chlorotrifluoromethylation of Alkynes: Synthesis of Tetrasubstituted Alkenes》 was published in Organic Letters. The article was written by Han, Hong Sik; Lee, Young Jin; Jung, Young-Sik; Han, Soo Bong. The article contains the following contents:

In the presence of fac-Ir(ppy)3 and Li2CO3 in acetone, trifluoromethanesulfonyl chloride added regioselectively and diastereoselectively to aryl alkynes such as 4-MeCONHC6H4CCMe under blue LED light to yield tetrasubstituted aryl trifluoromethyl alkenes such as I (R = Cl) in 34-85% yields and in all but one case as single diastereomers. I (R = Cl) underwent Suzuki coupling with aryl boronic acids or pinacolboronates to yield tetrasubstituted alkenes I (R = 4-EtOC6H4, 1-methyl-5-pyrazolyl, 3-furanyl, 2-benzothienyl) in 71-90% yields. The structure of a (tosylaminophenyl)chlorotrifluorobutene was determined by X-ray crystallog. The experimental part of the paper was very detailed, including the reaction process of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Recommanded Product: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

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, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Recommanded Product: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Yi, Rong-Nan; Wu, Zhi-Lin; Ouyang, Wen-Tao; Wang, Wei-Fan; He, Wei-Min published their research in Tetrahedron Letters on August 3 ,2021. The article was titled 《Green synthesis of 4-organylselanyl-1H-pyrazoles through electrochemical cross-dehydrogenative coupling of 1H-pyrazoles and diorganyl diselenides》.Formula: C4H6N2 The article contains the following contents:

An atom-economical and efficient method for synthesizing 4-organylselanyl-1H-pyrazoles through electrochem. cross-dehydrogenation coupling of N-unsubstituted pyrazoles with diorganyl diselenides under chem. oxidant-free and mild conditions was developed. This reaction not only shows good functional-group tolerance but also has high scalability. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpyrazole(cas: 930-36-9Formula: C4H6N2)

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. Formula: C4H6N2

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

In 2018,ACS Catalysis included an article by Boit, Timothy B.; Weires, Nicholas A.; Kim, Junyong; Garg, Neil K.. Recommanded Product: 847818-74-0. The article was titled 《Nickel-Catalyzed Suzuki-Miyaura Coupling of Aliphatic Amides》. The information in the text is summarized as follows:

Authors report the Ni-catalyzed Suzuki-Miyaura coupling of aliphatic amide derivatives Prior studies have shown that aliphatic amide derivatives can undergo Ni-catalyzed carbon-heteroatom bond formation but that Ni-mediated C-C bond formation using aliphatic amide derivatives has remained difficult. The coupling disclosed herein is tolerant of considerable variation with respect to both the amide-based substrate and the boronate coupling partner and proceeds in the presence of heterocycles and epimerizable stereocenters. Moreover, a gram-scale Suzuki-Miyaura coupling/Fischer indolization sequence demonstrates the ease with which unique polyheterocyclic scaffolds can be constructed, particularly by taking advantage of the enolizable ketone functionality present in the cross-coupled product. The methodol. provides an efficient means to form C-C bonds from aliphatic amide derivatives using nonprecious-metal catalysis and offers a general platform for the heteroarylation of aliphatic acyl electrophiles. In addition to this study using 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, there are many other studies that have used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Recommanded Product: 847818-74-0) was used in this study.

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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Recommanded Product: 847818-74-0

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

In 2019,Chemical Science included an article by Chong, Eugene; Qu, Bo; Zhang, Yongda; Cannone, Zachary P.; Leung, Joyce C.; Tcyrulnikov, Sergei; Nguyen, Khoa D.; Haddad, Nizar; Biswas, Soumik; Hou, Xiaowen; Kaczanowska, Katarzyna; Chwalba, Michal; Tracz, Andrzej; Czarnocki, Stefan; Song, Jinhua J.; Kozlowski, Marisa C.; Senanayake, Chris H.. Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. The article was titled 《A versatile catalyst system for enantioselective synthesis of 2-substituted 1,4-benzodioxanes》. The information in the text is summarized as follows:

The synthesis of enantiomerically enriched 1,4-benzodioxanes containing alkyl, aryl, heteroaryl and/or carbonyl substituents at the 2-position was reported. The starting 1,4-benzodioxines were readily synthesized via ring closing metathesis using an efficient nitro-Grela catalyst at ppm levels. Excellent enantioselectivities of up to 99:1 er were obtained by using the versatile catalyst system [Ir(cod)Cl]2/BIDIME-dimer in the asym. hydrogenation of 2-substituted 1,4-benzodioxines. Furthermore, DFT calculations revealed that the selectivity of the process was controlled by the protonation step; and coordinating groups on the substrate may alter the interaction with the catalyst, resulting in a change in the facial selectivity. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

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. Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Formula: C5H6N2O2In 1985 ,《N,N’-Linked biazoles. Part 5. Synthesis of pyrazolyl dimers by the reaction of 3-methoxycarbonyl-2-pyrazoline with lead tetraacetate》 appeared in Heterocycles. The author of the article were De Mendoza, Javier; Rosario Gonzalez-Muniz, M.; Rosario Martin, M.. The article conveys some information:

Depending on the reaction conditions, the title oxidation gave all products earlier reported and several new ones, e.g. I-III. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Formula: C5H6N2O2)

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.Formula: C5H6N2O2

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

In 1973,Akrem, A. A.; Kvasyuk, E. I.; Mikhailopulo, I. A. published 《Unusual reaction of 3-(methoxycarbonyl)-Δ2-pyrazoline with lead tetraacetate》.Tetrahedron Letters published the findings.Name: Methyl 1H-pyrazole-3-carboxylate The information in the text is summarized as follows:

The title reaction gave 70% 3-(methoxycarbonyl)-1-[1-(methoxycarbonyl)-cyclopropyl]pyrazole (I) and 14% 3-(methoxycarbonyl)-1-[3-(methoxycarbonyl)pyrazol-1-yl]-2-pyrazoline (II). NMR, ir, and uv spectral data for I, II, 3-(methoxycarbonyl)pyrazole, and 7-acetyl-3-(methoxycarbonyl)-2-pyrazoline were determined The experimental process involved the reaction of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Name: 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.Name: Methyl 1H-pyrazole-3-carboxylate

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

In 2015,Cheema, Hammad; Islam, Ashraful; Han, Liyuan; El-Shafei, Ahmed published 《Monodentate pyrazole as a replacement of labile NCS for Ru (II) photosensitizers: Minimum electron injection free energy for dye-sensitized solar cells》.Dyes and Pigments published the findings.Computed Properties of C4H3F3N2 The information in the text is summarized as follows:

A mono-dentate ligand of 3-(trifluoromethyl) pyrazole, instead of the labile isothiocyanate ligand for Ru (II) photosensitizers, was developed. This mol. modulation resulted in a new structure motif (HD-11) with 50 nm red shift in the low energy metal-to-ligand charge transfer (MLCT) absorption peak. However, electrochem. measurements revealed that both ground and excited state oxidation potentials were stabilized, this is attributed to the presence of strong electron withdrawing group CF3 tethered to pyrazole, which resulted in more free energy for dye regeneration, but less driving force for electron injection into the conduction band of TiO2. Hence HD-11, resulted in lower Jsc of 12.89 mA cm-2 compared to 17.07 mA cm-2 of N719 under similar conditions. Addnl., Voc of HD-11 was lower than N719, owing to decreased eTiO2 life time of 0.674 ms compared to 8.8 ms of N719 for injected electrons as found by impedance measurements. In addition to this study using 3-(Trifluoromethyl)-1H-pyrazole, there are many other studies that have used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Computed Properties of C4H3F3N2) was used in this study.

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.Computed Properties of C4H3F3N2

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

Formula: C4H3F3N2In 2020 ,《Pyrazole-Enaminones as Promising Prototypes for the Development of Analgesic Drugs》 appeared in ChemistrySelect. The author of the article were Moraes, Paulo A.; Brum, Evelyne S.; Brusco, Indiara; Marangoni, Mario A.; Lobo, Marcio M.; Camargo, Adriano F.; Nogara, Pablo A.; Bonacorso, Helio G.; Martins, Marcos A. P.; Da Rocha, Joao Batista T.; Oliveira, Sara M.; Zanatta, Nilo. The article conveys some information:

This study reports the chemo- and regioselective synthesis, at good yields, of (E)-4-(amino)-1,1,1-trifluoro-5-(4,5-alkyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)pent-3-en-2-ones (pyrazole-enaminones), from the of N-alkylation reaction of trifluoromethyl pyrazoles with 5-bromo enaminones. The obtained compounds were tested as potential analgesics in a screening test involving mice. Three of these compounds significantly reduced the spontaneous nociception induced by the application of capsaicin, which is an algogenic substance. Compound I presented satisfactory antinociceptive activity compared to celecoxib, a drug used as a pos. control, without promoting locomotor changes in the mice. Moreover, mol. modeling simulations showed that compound I interacts with the cyclooxygenase enzyme at the same binding site as celecoxib. Together, present data suggest that compound I is a promising prototype for the development of new analgesic drugs. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Formula: 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.Formula: C4H3F3N2

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