pyrazoles-derivatives

The N-alkylation and N-arylation of unsymmetrical pyrazoles was written by Grimmett, M. Ross;Lim, K. H. Richard;Weavers, Rex T.. And the article was included in Australian Journal of Chemistry in 1979.Synthetic Route of C4H5N3O2 This article mentions the following:

Unsym. pyrazoles with alkyl, aryl, nitro and carboxyl substituents at C-3 or C-5 were methylated with Me₂SO₄-MeOH, Me₂SO₂ in basic medium, and with CH₂N₂. The ratios of the isomeric N-methylpyrazoles were determined by NMR and gas liquid chromatog. The modified Ullmann phenylation was also applied to these pyrazoles. Product orientations involve considerations of electronic and steric effects, the possible intermediacy of quaternary salts, and the likelihood that the dominant tautomer is reacting. In the experiment, the researchers used many compounds, for example, 1-Methyl-3-nitro-1H-pyrazole (cas: 54210-32-1Synthetic Route of C4H5N3O2).

1-Methyl-3-nitro-1H-pyrazole (cas: 54210-32-1) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Synthetic Route of C4H5N3O2

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

Potent and Selective Ketoamide-Based Inhibitors of Cysteine Protease, Cathepsin K was written by Tavares, Francis X.;Deaton, David N.;Miller, Aaron B.;Miller, Larry R.;Wright, Lois L.;Zhou, Hui-Qiang. And the article was included in Journal of Medicinal Chemistry in 2004.Application In Synthesis of 1-Ethyl-1H-pyrazol-5-amine This article mentions the following:

Cathepsin K, a lysosomal cysteine protease of the papain superfamily, is abundantly and selectively expressed in osteoclasts, suggesting that this enzyme is crucial for bone resorption. Prevention of osteoclast-mediated bone resorption via inhibition of cathepsin K could be an effective approach to prevent osteoporosis. Potent and selective reversible ketoamide-based inhibitors have been identified in the present study. Using a known crystal structure of a ketoamide-based inhibitor, information from residues that form the P2/P3 pocket was used in the design of inhibitors that could allow for gains in selectivity and potency. Further, incorporation of P’ selective heterocycles, along with the P2/P3 modifications, is also described. These modifications have resulted in potent and selective cathepsin K inhibitors that allow for improvements in their physiochem. properties and represent a viable lead series for the discovery of new therapies for the prevention and treatment of osteoporosis. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Application In Synthesis of 1-Ethyl-1H-pyrazol-5-amine).

1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. Pyrazoles, a five-membered heterocycle containing two adjacent nitrogen atoms, are the core structures found in a number of molecules that possess a wide range of pharmaceutical and agricultural activities. Pyrazoles and pyrimidines have diverse biological and pharmacological activities. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Pyrazofurin is important antimicrobial drug and 2-methylpyrimidine-4-ylamine derivatives I and II were found to be effective inhibitors of Escherichia coli PDHc-E1 with antibacterial and antifungal activity.Application In Synthesis of 1-Ethyl-1H-pyrazol-5-amine

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

Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor was written by Zhao, Yujun;Zhou, Bing;Bai, Longchuan;Liu, Liu;Yang, Chao-Yie;Meagher, Jennifer L.;Stuckey, Jeanne A.;McEachern, Donna;Przybranowski, Sally;Wang, Mi;Ran, Xu;Aguilar, Angelo;Hu, Yang;Kampf, Jeff W.;Li, Xiaoqin;Zhao, Ting;Li, Siwei;Wen, Bo;Sun, Duxin;Wang, Shaomeng. And the article was included in Journal of Medicinal Chemistry in 2018.Quality Control of 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine This article mentions the following:

We report the structure-based discovery of CF53 (28) as a highly potent and orally active inhibitor of bromodomain and extra-terminal (BET) proteins. By the incorporation of a NH-pyrazole group into the 9H-pyrimido[4,5-b]indole core, we identified a series of compounds that bind to BRD4 BD1 protein with K_i values of <1 nM and achieve low nanomolar potencies in the cell growth inhibition of leukemia and breast cancer cells. The most-promising compound, CF53, possesses excellent oral pharmacokinetic properties and achieves significant antitumor activity in both triple-neg. breast cancer and acute leukemia xenograft models in mice. Determination of the co-crystal structure of CF53 with the BRD4 BD1 protein provides a structural basis for its high binding affinity to BET proteins. CF53 is very selective over non-BET bromodomain-containing proteins. These data establish CF53 as a potent, selective, and orally active BET inhibitor, which warrants further evaluation for advanced preclin. development. In the experiment, the researchers used many compounds, for example, 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine (cas: 141459-53-2Quality Control of 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine).

1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine (cas: 141459-53-2) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Quality Control of 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine

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

Platinum(II) and palladium(II) complexes with 3,5-dimethyl-1-pyrazolylcarbamide was written by Safronova, L. A.;Shebaldova, A. D.. And the article was included in Koordinatsionnaya Khimiya in 1989.Recommanded Product: 3,5-Dimethyl-1H-pyrazole-1-carboxamide This article mentions the following:

MLCl₂ (M = Pd, Pt; L = 3,5-dimethyl-1-pyrazolylcarbamide) were prepared and characterized by IR and ¹H NMR spectra and colorimetry with SnCl₂. L coordinates through the pyridine N atom and the amino N atom. In the experiment, the researchers used many compounds, for example, 3,5-Dimethyl-1H-pyrazole-1-carboxamide (cas: 934-48-5Recommanded Product: 3,5-Dimethyl-1H-pyrazole-1-carboxamide).

3,5-Dimethyl-1H-pyrazole-1-carboxamide (cas: 934-48-5) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. Pyrazoles and pyrimidines have diverse biological and pharmacological activities. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Pyrazofurin is important antimicrobial drug and 2-methylpyrimidine-4-ylamine derivatives I and II were found to be effective inhibitors of Escherichia coli PDHc-E1 with antibacterial and antifungal activity.Recommanded Product: 3,5-Dimethyl-1H-pyrazole-1-carboxamide

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

Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors was written by Moree, Wilna J.;Goldman, Phyllis;Demaggio, Anthony J.;Christenson, Erik;Herendeen, Dan;Eksterowicz, John;Kesicki, Edward A.;McElligott, David L.;Beaton, Graham. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Name: 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine This article mentions the following:

A novel class of PARP-1 inhibitors was identified containing a non-aromatic heterocycle or carbocycle fused to a pyrazolo pyridin-2-one. Compounds displayed low nanomolar binding activity in the PARP-1 binding assay and submicromolar activity in a cell based chemosensitization assay. In the experiment, the researchers used many compounds, for example, 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine (cas: 141459-53-2Name: 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine).

1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine (cas: 141459-53-2) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple 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.Name: 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine

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

High Throughput Synthesis of Extended Pyrazolo[3,4-d]dihydropyrimidines was written by Ryabukhin, Sergey V.;Granat, Dmitry S.;Plaskon, Andrey S.;Shivanyuk, Alexander N.;Tolmachev, Andrey A.;Volovenko, Yulian M.. And the article was included in ACS Combinatorial Science in 2012.Electric Literature of C8H15N3 This article mentions the following:

Fused pyrazolo[3,4-d]pyrimidines such as I (R = Ph, 4-MeOC₆H₄, 4-ClC₆H₄, 5-phenyl-2-furanyl, 1-phenyl-4-pyrazolyl, 3,4-Me₂C₆H₃, 3-F₃CC₆H₄, 3-Me-2-thienyl, 3-ClC₆H₄, 5-Me-2-furanyl, 3,5-dimethyl-4-isoxazolyl, 3,4-Cl₂C₆H₃, 2-FC₆H₄, 3-FC₆H₄, 4-Me₂NC₆H₄, 2-F₂CHOC₆H₄; R¹ = H; R² = H, F₃C, Me₂NSO₂, 1-pyrrolidinylsulfonyl, 1-piperidinylsulfonyl, 4-morpholinylsulfonyl; R¹R² = benzo) were prepared in two steps from 1-substituted-5-pyrazoleamines such as 1-isopropyl-5-pyrazoleamine, heteroaryl chlorides such as 2-chloropyridine, and aldehydes such as benzaldehyde. N-heteroaryl 5-pyrazoleamines such as II (R¹ = H; R² = H, F₃C, 1-piperidinylsulfonyl; R¹R² = benzo) were generated by base-mediated condensation of 5-pyrazoleamines such as 1-phenyl-3-methyl-5-pyrazoleamine with heteroaryl chlorides such as 2-chloropyridine; heating the heteroaryl pyrazoleamines with aryl aldehydes or isatins either in a sealed tube with trimethylsilyl chloride or in glacial acetic acid followed by crystallization yielded pyrazolo[3,4-d]pyrimidines. Reaction of N-heteroaryl 5-pyrazoleamines with cyclohexanone provided N-heteroaryl 4-(1-cyclohexen-1-yl)-5-pyrazoleamines rather than spirocyclohexanepyrazolopyrimidines. A library of > 200 pyrazolo[3,4-d]pyrimidines were prepared; the distribution of the library members within ranges of lipophilicity, mol. weight, hydrogen bond acceptor and donor count, and polar surface area was determined In the experiment, the researchers used many compounds, for example, 1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine (cas: 141459-53-2Electric Literature of C8H15N3).

1-(tert-Butyl)-3-methyl-1H-pyrazol-5-amine (cas: 141459-53-2) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles and pyrimidines have diverse biological and pharmacological activities. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Pyrazofurin is important antimicrobial drug and 2-methylpyrimidine-4-ylamine derivatives I and II were found to be effective inhibitors of Escherichia coli PDHc-E1 with antibacterial and antifungal activity.Electric Literature of C8H15N3

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

Mass spectrometry of nitroazoles. I. The mass spectra of methyl substituted nitropyrazoles was written by Luijten, W. C. M. M.;Van Thuijl, J.. And the article was included in Organic Mass Spectrometry in 1979.Category: pyrazoles-derivatives This article mentions the following:

The mass spectra of all isomers of methylnitropyrazoles are reported. Generally, the spectra are characteristic of nitropyrazoles. In some cases however, ortho effects occur, which were recognizable by the primary loss of •OH, H₂O, •CHO and HCHO. In the experiment, the researchers used many compounds, for example, 1-Methyl-3-nitro-1H-pyrazole (cas: 54210-32-1Category: pyrazoles-derivatives).

1-Methyl-3-nitro-1H-pyrazole (cas: 54210-32-1) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Category: pyrazoles-derivatives

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

Rhodium(III)-Catalyzed Oxidative Coupling of 5-Aryl-1H-pyrazoles with Alkynes and Acrylates was written by Li, Xingwei;Zhao, Miao. And the article was included in Journal of Organic Chemistry in 2011.Safety of 3-(4-Bromophenyl)-1H-pyrazole This article mentions the following:

[RhCp*Cl₂]₂-catalyzed oxidative coupling of 5-aryl-1H-pyrazoles with alkynes and acrylates has been achieved using Cu(OAc)₂ as an oxidant. Coupling with alkynes afforded six-membered azacycles, e.g., I, as a result of C-C and C-N coupling. Coupling with acrylates followed a process of diolefination and a subsequent aza-Michael cyclization. In the experiment, the researchers used many compounds, for example, 3-(4-Bromophenyl)-1H-pyrazole (cas: 73387-46-9Safety of 3-(4-Bromophenyl)-1H-pyrazole).

3-(4-Bromophenyl)-1H-pyrazole (cas: 73387-46-9) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns.Safety of 3-(4-Bromophenyl)-1H-pyrazole

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

One-pot Synthesis of Substituted Pyrazoles from Propargyl Alcohols via Cyclocondensation of in situ-Generated α-Iodo Enones/Enals and Hydrazine Hydrate was written by Guo, Huifeng;Zhang, Qinglin;Pan, Wanyong;Yang, Hong;Pei, Keke;Zhai, Jiulong;Li, Tiantian;Wang, Zhihai;Wang, Yan;Yin, Yan. And the article was included in Asian Journal of Organic Chemistry in 2021.COA of Formula: C9H7BrN2 This article mentions the following:

An efficient Bi(OTf)₃-catalyzed transformation of unprotected propargylic alcs. has been developed, affording a general, one-pot approach to access diverse pyrazoles via sequential iodo-intercepted Meyer-Schuster rearrangement, cyclocondensation of NH₂NH₂·H₂O and α-iodo enones/enals generated in situ, and iodine elimination. This transformation tolerates a wide range of substrates and is reliable on a large scale. The high yields and convenient exptl. operations make it a valuable method for the construction of pyrazole derivatives In the experiment, the researchers used many compounds, for example, 3-(4-Bromophenyl)-1H-pyrazole (cas: 73387-46-9COA of Formula: C9H7BrN2).

3-(4-Bromophenyl)-1H-pyrazole (cas: 73387-46-9) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns.COA of Formula: C9H7BrN2

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

Investigation of thermal stability of high-melting thermostable explosives was written by Falyakhov, I. F.;Sharnin, G. P.;Safin, N. M.;Saifullin, I. Sh.;Fassakhov, R. Kh.. And the article was included in Proceedings of the International Pyrotechnics Seminar in 1995.Electric Literature of C4H5N3O2 This article mentions the following:

The kinetics is studied of thermal decomposition of aromatic and heteroaromatic organic compounds and their salts. The thermal stability is studied of high-melting explosives, nitro derivatives of aromatic and heteroaromatic organic compounds (nitropyrroles, nitroimidazoles, nitropyrazoles, nitro derivatives of 1,2,4-triazoles, nitropyridines and their metal salts, benzofurazanes and benzofuroxanes). In the experiment, the researchers used many compounds, for example, 1-Methyl-3-nitro-1H-pyrazole (cas: 54210-32-1Electric Literature of C4H5N3O2).

1-Methyl-3-nitro-1H-pyrazole (cas: 54210-32-1) belongs to pyrazole derivatives. Pyrazole has two ring nitrogen atoms in which N1 is pyrrolic and N2 is pyridine-like. The N1 nitrogen is not reactive but is deprotonated in the presence of a base-forming anion. 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.Electric Literature of C4H5N3O2

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