Category: 20154-03-4

Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazoleIn 2019 ,《Chemo- and regioselective reactions of 5-bromo enones/enaminones with pyrazoles》 was published in Organic & Biomolecular Chemistry. The article was written by Moraes, Paulo A.; Lobo, Marcio M.; Marangoni, Mario A.; Meyer, Alexandre R.; Frizzo, Clarissa P.; Bonacorso, Helio G.; Martins, Marcos A. P.; Zanatta, Nilo. The article contains the following contents:

Reaction of 5-bromo enones with pyrazoles provided a series of unexpected N,O-aminal derivatives, I [Y = Me, CF3; R1 = H, Me; R2 = H, Me, n-Pr, etc.; R3 = Me, Et, n-Pr, n-Bu; R1R2 = (CH2)3, (CH2)4] through a 1,4-conjugated addition at the β-carbon of the 5-bromo enones instead of the expected nucleophilic substitution of the bromine. This reaction also furnished the 1,3-regioisomer of the pyrazole. A similar reaction of pyrazoles using 5-bromo enaminones furnished only N-alkylated pyrazoles II [R4 = Me, i-Bu, (CH2)4, etc.] with high regioselectivity and at good yields through nucleophilic substitution of the bromine. In the part of experimental materials, we found many familiar compounds, such as 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

Nale, Sagar D.; Thombal, Raju S.; Lee, Yong Rok published their research in Asian Journal of Organic Chemistry in 2021. The article was titled 《Ruthenium(II)-Catalyzed Direct Ortho Functionalization of 1-Arylpyrazoles with Maleimides: A Condition Controlled Installation of Succinimides and Maleimides on Arenes》.Electric Literature of C4H3F3N2 The article contains the following contents:

Ruthenium(II)-catalyzed switchable ortho functionalization of 1-arylpyrazoles I (R1 = 2-Me, 4-OMe, 4-Cl, etc.; R2 = H, Me, CF3) and 1-(1-naphthalenyl)-1H-pyrazole with maleimides II (R3 = C2H5, C6H5, 4-BrC6H4, etc.) is developed in this study. This divergent reaction proceeds via five-membered ruthenacycle formation and selectively installs diverse succinimides III (R4 = 3-Me, 5-OMe, 5-Cl, etc.) and maleimides IV substituents on the aromatic ring of 1-arylpyrazoles I through alkylation and alkenylation under acidic and basic conditions. This methodol. features broad substrate scope, high functional group tolerance, selective functionalization, and superior reactivity. The experimental part of the paper was very detailed, including the reaction process of 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

《Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma》 was written by Chen, Yun; Bai, Gang; Ning, Yi; Cai, Shi; Zhang, Tao; Song, Peiran; Zhou, Jinpei; Duan, Wenhu; Ding, Jian; Xie, Hua; Zhang, Huibin. Quality Control of 3-(Trifluoromethyl)-1H-pyrazole And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

The design, synthesis and structure-activity relationships of imidazo[1,2-b]pyridazines I [R = 2-aminoethyl, 3-amino-piperidin-1-yl, piperazin-1-yl, etc.; R1 = CF2, CF3, CN, etc.; R2 =Me, Et, iPr, etc.; R3 = H, Me] as potent IRAK4 inhibitors was reported. The representative compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] exhibited excellent IRAK4 potency (IRAK4 IC50 = 1.3 nM) and favorable kinase selectivity profile. It demonstrated cellular selectivity for activated B cell-like (ABC) subtype DLBCL with MYD88 L265P mutation in cytotoxicity assay. The kinase inhibitory efficiency of compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] was further validated by western blot anal. of phosphorylation of IRAK4 and downstream signaling in OCI-LY10 and TMD8 cells. Besides, combination of compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] and BTK inhibitor ibrutinib synergistically reduced the viability of TMD8 cells. These results indicated that compound I [R = amino-piperidin-3-yl; R1 = CF2; R2 = Me; R3 = H] could be a promising IRAK4 inhibitor for the treatment of mutant MYD88 DLBCL. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Quality Control of 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.Quality Control of 3-(Trifluoromethyl)-1H-pyrazole

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

In 2016,Petrella, Stephanie; Aubry, Alexandra; Janvier, Genevieve; Coutant, Eloi P.; Cartier, Alex; Dao, Thuy-Ha; Bonhomme, Frederic J.; Motreff, Laurence; Pissis, Cedric; Bizet, Chantal; Clermont, Dominique; Begaud, Evelyne; Retailleau, Pascal; Munier-Lehmann, Helene; Capton, Estelle; Mayer, Claudine; Janin, Yves L. published 《Synthesis and evaluation of original bioisosteres of bacterial type IIA topoisomerases inhibitors》.Canadian Journal of Chemistry published the findings.SDS of cas: 20154-03-4 The information in the text is summarized as follows:

A recently discovered series of inhibitors of the ATPase function of bacterial type IIA topoisomerases featuring a carboxypyrrole component led the authors to attempt to replace this group with a potentially bioisosteric carboxypyrazole. Accordingly, synthetic pathways to 2-(4-(1H-pyrazole-5-carboxamido)piperidin-1-yl)thiazole-5-carboxylic acids or 2-(4-(N-methyl-1H-pyrazole-5-carboxamido)piperidin-1-yl)thiazole-5-carboxylic acids featuring an array of substituents on the pyrazole ring were explored. Unfortunately, none of the analogs made were effective on the ATPase function of Mycobacterium tuberculosis gyrase as well on the DNA supercoiling activity of the whole gyrase of M. tuberculosis and Escherichia coli. However, this work is still providing original insights in chem. as well as in the structure-activity relationships of this series of inhibitors. In addition to this study using 3-(Trifluoromethyl)-1H-pyrazole, there are many other studies that have used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4SDS of cas: 20154-03-4) 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.SDS of cas: 20154-03-4

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

In 2012,Bhanuchandra, M.; Kuram, Malleswara Rao; Sahoo, Akhila K. published 《A convenient approach to β-heteroarylated (C-N bond) ketones from Cs2CO3 promoted reaction between propargyl alcohols and nitrogen-heterocycles》.Organic & Biomolecular Chemistry published the findings.Synthetic Route of C4H3F3N2 The information in the text is summarized as follows:

An efficient and direct approach to β-heteroarylated (C-N bond) ketones is demonstrated. Base promoted redox isomerization of propargyl alc. to α,β-unsaturated ketone followed by conjugate addition to NH-heteroarenes affords a wide range of β-heteroarylated ketones in good to excellent yields. Aryl, heteroaryl, alkyl C(sp), and terminal alkynes containing unactivated propargyl alcs. effectively undergo redox-isomerization conjugate addition (RICA) with NH-heteroarenes. Reaction of 3-substituted pyrazoles or indazole with propargyl alcs. enables highly regioselective products. A diverse range of NH-bearing nucleophiles such as: pyrazoles, imidazole, triazoles, pyrrole, indoles, and aniline participate in this reaction and deliver the corresponding β-heteroarylated ketones. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Synthetic Route 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.Synthetic Route of C4H3F3N2

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

Synthetic Route of C4H3F3N2In 2021 ,《Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE)》 was published in Journal of Medicinal Chemistry. The article was written by Kotian, Pravin L.; Wu, Minwan; Vadlakonda, Satish; Chintareddy, Venkat; Lu, Pengcheng; Juarez, Luis; Kellogg-Yelder, Debra; Chen, Xilin; Muppa, Saritha; Chambers-Wilson, Ramanda; Davis Parker, Cynthia; Williams, Jason; Polach, Kevin J.; Zhang, Weihe; Raman, Krishnan; Babu, Yarlagadda S.. The article contains the following contents:

Hereditary angioedema (HAE) is a rare and potentially life-threatening disease that affects an estimated 1 in 50 000 individuals worldwide. Until recently, prophylactic HAE treatment options were limited to injectables, a burdensome administration route that has driven the need for an oral treatment. A substantial body of evidence has shown that potent and selective plasma kallikrein inhibitors that block the generation of bradykinin represent a promising approach for the treatment of HAE. Berotralstat (BCX7353, discovered by BioCryst Pharmaceuticals using a structure-guided drug design strategy) is a synthetic plasma kallikrein inhibitor that is potent and highly selective over other structurally related serine proteases. This once-daily, small-mol. drug is the first orally bioavailable prophylactic treatment for HAE attacks, having successfully completed a Phase III clin. trial (meeting its primary end point) and recently receiving the U.S. Food and Drug Administration’s approval for the prophylactic treatment of HAE attacks in patients 12 years and older. In the experiment, the researchers used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Synthetic Route 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.Synthetic Route of C4H3F3N2

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

Application of 20154-03-4In 2021 ,《Metal-Free Direct Oxidative C-N Bond Coupling of Quinoxalin-2(1H)-ones with Azoles under Mild Conditions》 appeared in European Journal of Organic Chemistry. The author of the article were Guo, Jingwen; Zhang, Lina; Du, Xinyue; Zhang, Liting; Cai, Yuepiao; Xia, Qinqin. The article conveys some information:

Direct C3-H amination of quinoxalin-2(1H)-ones with azoles under mild conditions promoted by PIFA has been achieved in good yield in a very fast manner. Mechanistic study revealed that the reaction proceeds through a radical process. In addition, this method could be applied to gram-scale reaction.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application 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.Application of 20154-03-4

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

Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazoleIn 2010 ,《Selective angiotensin II AT2 receptor agonists with reduced CYP 450 inhibition》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Mahalingam, A. K.; Wan, Yiqian; Murugaiah, A. M. S.; Wallinder, Charlotta; Wu, Xiongyu; Plouffe, Bianca; Botros, Milad; Nyberg, Fred; Hallberg, Anders; Gallo-Payet, Nicole; Alterman, Mathias. The article conveys some information:

Structural alterations to the benzylic position of the first drug-like selective angiotensin II AT2 receptor agonist (1) have been performed, with the emphasis to reduce the CYP 450 inhibitory property of the initial structure. The imidazole moiety, responsible for the CYP 450 inhibitory effect in 1, was replaced with various heterocycles. In addition, the modes of attachment of the heterocycles, i.e., carbon vs. nitrogen attachment, and introduction of carbonyl functionalities to the benzylic position have been evaluated. In all the three series, AT2 receptor ligands with affinity in the lower nanomolar range were identified. None of the analogs, regardless of the substituents, exhibited any affinity for the AT1 receptor. Compounds with substantially reduced inhibition of the CYP 450 enzymes were obtained. Among them the compound 60 was found to induce neurite elongation in NG 108-15 cells and served as potent AT2 selective agonist.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole) 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.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole

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

In 2012,Srinivas, Dharavath; Ghule, Vikas D.; Tewari, Surya P.; Muralidharan, Krishnamurthi published 《Synthesis of Amino, Azido, Nitro, and Nitrogen-Rich Azole Substituted Derivatives of 1H-Benzotriazole for High-Energy Materials Applications》.Chemistry – A European Journal published the findings.Recommanded Product: 20154-03-4 The information in the text is summarized as follows:

The amino, azido, nitro, and nitrogen-rich azole substituted derivatives of 1H-benzotriazole were synthesized for energetic material applications. The synthesized compounds were fully characterized by 1H and 13C NMR spectroscopy, IR, MS, and elemental anal. 5-Chloro-4-nitro-1H-benzo[1,2,3]triazole and 5-azido-4,6-dinitro-1H-benzo[1,2,3]triazole crystallize in the Pca21 (orthorhombic) and P21/c (monoclinic) space group, resp., as determined by single-crystal X-ray diffraction. Their densities are 1.71 and 1.77 g cm-3, resp. The calculated densities of the other compounds range between 1.61-1.98 g cm-3. The detonation velocity values calculated for these synthesized compounds range from 5.45-8.06 km s-1, and the detonation pressure ranges from 12.35-28 GPa.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Recommanded Product: 20154-03-4) 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.Recommanded Product: 20154-03-4

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

In 2012,Murugaiah, A. M. S.; Wu, Xiongyu; Wallinder, Charlotta; Mahalingam, A. K.; Wan, Yiqian; Skoeld, Christian; Botros, Milad; Guimond, Marie-Odile; Joshi, Advait; Nyberg, Fred; Gallo-Payet, Nicole; Hallberg, Anders; Alterman, Mathias published 《From the First Selective Non-Peptide AT2 Receptor Agonist to Structurally Related Antagonists》.Journal of Medicinal Chemistry published the findings.Product Details of 20154-03-4 The information in the text is summarized as follows:

A para substitution pattern of the Ph ring is a characteristic feature of the first reported selective AT2 receptor agonist M024/C21 (1) and all the nonpeptidic AT2 receptor agonists described so far. Two series of compounds structurally related to 1 but with a meta substitution pattern have now been synthesized and biol. evaluated for their affinity to the AT1 and AT2 receptors. A high AT2/AT1 receptor selectivity was obtained with all 41 compounds synthesized, and the majority exhibited Ki ranging from 2 to 100 nM. Five compounds were evaluated for their functional activity at the AT2 receptor, applying a neurite outgrowth assay in NG108-15 cells. Notably, four of the five compounds, with representatives from both series, acted as potent AT2 receptor antagonists. These compounds were found to be considerably more effective than PD 123,319, the standard AT2 receptor antagonist used in most laboratories No AT2 receptor antagonists were previously reported among the derivatives with a para substitution pattern. Hence, by a minor modification of the agonist 1 it could be transformed into the antagonist, compound 38. These compounds should serve as valuable tools in the assessment of the role of the AT2 receptor in more complex physiol. models. 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. 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.Product Details of 20154-03-4

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