Category: 2075-46-9

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Computed Properties of 2075-46-9.

He, Yali;Hwang, Dong-Jin;Ponnusamy, Suriyan;Thiyagarajan, Thirumagal;Mohler, Michael L.;Narayanan, Ramesh;Miller, Duane D. research published 《 Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer》, the research content is summarized as follows. We report herein the design, synthesis, and pharmacol. characterization of a library of novel aryl pyrazol-1-yl-propanamides as selective androgen receptor degraders (SARDs) and pan-antagonists that exert broad-scope AR antagonism. Pharmacol. evaluation demonstrated that introducing a pyrazole moiety as the B-ring structural element in the common A-ring-linkage-B-ring nonsteroidal antiandrogens’ general pharmacophore allowed the development of a new scaffold of small mols. with unique SARD and pan-antagonist activities even compared to our recently published AF-1 binding SARDs such as UT-155 and UT-34. Novel B-ring pyrazoles exhibited potent AR antagonist activities, including promising distribution, metabolism, and pharmacokinetic properties, and broad-spectrum AR antagonist properties, including potent in vivo antitumor activity. I was able to induce an 80% tumor growth inhibition of xenografts derived from the enzalutamide-resistant (Enz-R) VCaP cell line. These results represent an advancement toward the development of novel AR antagonists for the treatment of Enz-R prostate cancer.

Computed Properties of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Formula: C3H3N3O2.

Hillrichs, Kai;Namyslo, Jan C.;Lederle, Felix;Huebner, Eike G.;Schmidt, Andreas research published 《 Pyrazoles in the Intersection of Mesomeric Betaines and N-Heterocyclic Carbenes: Formation of NHC Selenium Adducts of Pyrazolium-4-aminides》, the research content is summarized as follows. Starting from 4-nitropyrazole, eight mesoionic pyrazolium-4-aminides I (R = Me, Ph; R¹ = Ph, Et, c-Pr, etc.) were prepared by a six-step reaction sequence. The deprotonation of 1,2-disubstituted 4-amido-1H-pyrazolium salts by an anion exchange resin in its hydroxide form is the final step of the synthesis. A tautomeric equilibrium between the mesoionic compounds (pyrazolium-4-aminides) and N-heterocyclic carbenes (pyrazol-3-ylidenes) can be formulated. Apart from tautomerism, anionic N-heterocyclic carbenes can be formulated as a result of a deprotonation of the mesoionic compounds Trapping reactions were performed with selenium, which resulted in the formation of pyrazole-3-selenones II (R = Me, Ph; R¹ = Ph, Et, c-Pr, ete.). Methylation at the selenium atom gave the corresponding 3-(methylselanyl)-4-amido-1H-pyrazolium salts, which were deprotonated to give new mesomeric betaines, 3-(methylselanyl)-1H-pyrazolium-4-aminides III as unique compounds

Formula: C3H3N3O2, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Electric Literature of 2075-46-9.

Ghosh, Tubai;Maity, Pintu;Ranu, Brindaban C. research published 《 Cobalt-Copper Catalyzed C(sp2) – N Cross Coupling of Amides or Nitrogenated Heterocycles with Styrenyl or Aryl Halides》, the research content is summarized as follows. An efficient C(sp2)-N-cross coupling of cyclic and acyclic amides with styrenyl/aryl/heteroaryl halides catalyzed by cobalt acetylacetonate in combination with copper(I) iodide was achieved. A library of diversely substituted cyclic and acyclic enamides were obtained in high yields by this procedure. The reaction was stereoselective producing (E)-enamides from trans-styrenyl halides and (Z)-products from cis-halides. This procedure was successfully employed for the coupling of other N-heterocycles such as pyrazole, imidazole and triazole with aryl/styrenyl/heteroaryl halides to produce the corresponding N-coupled products. A probable mechanism was suggested.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., Electric Literature of 2075-46-9

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Formula: C3H3N3O2.

Glinkerman, Christopher M.;Boger, Dale L. research published 《 Synthesis, Characterization, and Rapid Cycloadditions of 5-Nitro-1,2,3-triazine》, the research content is summarized as follows. The synthesis, characterization, and a study of the cycloaddition reactions of 5-nitro-1,2,3-triazine (I) are reported. The electron-deficient nature of I permits rapid cycloaddition with a variety of electron-rich dienophiles, including amidines, enamines, enol ethers, ynamines, and ketene acetals in high to moderate yields. ¹H NMR studies of a representative cycloaddition reaction between I and an amidine revealed a remarkable reaction rate and efficiency (1 mM, <60 s, CD₃CN, 23°, >95%).

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., Formula: C3H3N3O2

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Application In Synthesis of 2075-46-9.

Goi, Takashi;Fukase, Koichi research published 《 Highly Efficient Coupling of Unstable Bicyclic Pyrimidines and Pyrazoles under Basic Conditions, and its Application to the Synthesis of Pharmaceutical Compounds》, the research content is summarized as follows. The efficient Pd-catalyzed coupling of unstable bicyclic pyrimidines and pyrazoles under basic conditions was established for the first time. The reactions proceeded with excellent yields without hydrolysis using Pd₂(dba)₃, ^tBuXPhos, and K₃PO₄.

Application In Synthesis of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Name: 4-Nitro-1H-pyrazole.

Guyot, Laetitia;Simon, Florian;Garcia, Jessica;Vanhalle, Floriane;Vilchez, Gaelle;Bardel, Claire;Manship, Brigitte;Puisieux, Alain;Machon, Christelle;Jacob, Guy;Guitton, Jerome;Payen, Lea research published 《 Structure-activity relationship study: Mechanism of cyto-genotoxicity of Nitropyrazole-derived high energy density materials family》, the research content is summarized as follows. Stringent toxicol. tests have to be performed prior to the industrial development of alternative chems. particularly high energy dense materials (HEDMs) such as explosives. The properties (e.g., power, stability) of these compounds are constantly being improved, the current axis of research being the nitration of nitrogen heterocycles leading to HEDMs such as nitropyrazole-derived mols. However, except for 3,4,5-trinitropyrazole (3,4,5-TNP), which was shown to be highly toxic in mice, the toxicol. impact of these HEDMs has so far not been investigated. Furthermore, as industrials are strongly advised to develop alternative safety testing assays to in vivo experiments, we herein focused on determining the cytotoxic and genotoxic effects of seven Nitropyrazole-derived HEDMs on three rodent cell lines (mouse embryonic BALB/3T3 clone A31 cells, Chinese hamster ovary cells CHO-K1 and mouse lymphoma L5178Y TK +/- clone (3.7.2C) cells), two human fibroblast lines (CRC05, PFS04062) and on the human hepatic HepaRG model (both in proliferative and differentiated cells). A stronger cytotoxic effect was observed for 1,3-dinitropyrazole (1, 3-DNP) and 3,4,5-TNP in all cell lines, though differentiated HepaRG cells clearly displayed fewer likely due to the metabolism and elimination of these mols. by their functional biotransformation pathways. At the mechanistic level, the sub-chronic cytotoxic and genotoxic effects were linked to ROS/RNS production (exptl. assays), HA2. X and to transcriptomic data highlighting the increase in DNA repair mechanisms.

Name: 4-Nitro-1H-pyrazole, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. COA of Formula: C3H3N3O2.

Feng, Pengju;Ma, Guojian;Chen, Xiaoguang;Wu, Xing;Lin, Ling;Liu, Peng;Chen, Tianfeng research published 《 Electrooxidative and Regioselective C-H Azolation of Phenol and Aniline Derivatives》, the research content is summarized as follows. A general and practical protocol was developed for the regioselective C-H azolation of phenol and aniline derivatives by electrooxidative cross-coupling [e.g., 4-methoxyphenol + pyrazole → 4-methoxy-2-(1H-pyrazol-1-yl)phenol (97%)]. The reaction occurs under metal-, oxidant-, and reagent-free conditions, allowing access to a wide variety of synthetically useful heteroarene derivatives The reaction also tolerates a broad range of functional groups and is amenable to gram-scale synthesis. Finally, a preliminary mechanistic study indicated that a radical-radical-combination pathway might be involved in the coupling reaction.

COA of Formula: C3H3N3O2, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Computed Properties of 2075-46-9.

Feng, Yangbo;Park, HaJeung;Bauer, Luke;Ryu, Jae Cheon;Yoon, Sung Ok research published 《 Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors》, the research content is summarized as follows. Potent JNK3 isoform selective inhibitors were developed from a thiophenyl-pyrazolourea scaffold. Through structure activity relationship (SAR) studies utilizing enzymic and cell-based assays, and in vitro and in vivo drug metabolism and pharmacokinetic (DMPK) studies, potent and highly selective JNK3 inhibitors with oral bioavailability and brain penetrant capability were developed. Inhibitor 17 was a potent and isoform selective JNK3 inhibitor (IC₅₀ = 35 nM), had significant inhibition to only JNK3 in a panel profiling of 374 wild-type kinases, had high potency in functional cell-based assays, had high stability in human liver microsome (t_1/2 = 66 min) and a clean CYP-450 inhibition profile, and was orally bioavailable and brain penetrant. Moreover, cocrystal structures of compounds 17 and 27 in human JNK3 were solved at 1.84 Å, which showed that these JNK3 isoform selective inhibitors bound to the ATP pocket, had interactions in both hydrophobic pocket-I and hydrophobic pocket-II.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., Computed Properties of 2075-46-9

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Computed Properties of 2075-46-9.

Fernandez, Belen;Fernandez, Ignacio;Cepeda, Javier;Medina-ODonnell, Marta;Rufino-Palomares, Eva E.;Raya-Baron, Alvaro;Gomez-Ruiz, Santiago;Perez-Jimenez, Amalia;Lupianez, Jose Antonio;Reyes-Zurita, Fernando J.;Rodriguez-Dieguez, Antonio research published 《 Modulating Anticancer Potential by Modifying the Structural Properties of a Family of Zinc Metal-Organic Chains Based on 4-Nitro-1H-pyrazole》, the research content is summarized as follows. The authors synthesized a novel family of metal-organic chains based on 4-nitro-1H-pyrazole linker and zinc as metal center. The authors report the formation of these coordination polymers using hydrothermal routes with water as solvent. These materials display one-dimensional structures with major structural modifications from minimal synthetic variations. What is more interesting, the authors have carried out antitumor measurements, and the authors have related these properties with the structural networks. To the best of the authors’ knowledge, these materials constitute the first examples of polymeric structures for 4-NO₂-pz ligands. NMR and MS spectrometry were used to verify the characterization of the metal complexes in solution to corroborate that these materials are present in the biol. assays.

Computed Properties of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Safety of 4-Nitro-1H-pyrazole.

Fleuti, Marianne;Bartova, Katerina;Slavetinska, Lenka Postova;Tloust’ova, Eva;Tichy, Michal;Gurska, Sona;Pavlis, Petr;Dzubak, Petr;Hajduch, Marian;Hocek, Michal research published 《 Synthesis and Biological Profiling of Pyrazolo-Fused 7-Deazapurine Nucleosides》, the research content is summarized as follows. A series of 8-substituted 1-methyl-1,4-dihydropyrazolo[3′,4′:4,5]pyrrolo[2,3-d]pyrimidine (methylpyrazolo-fused 7-deazapurine) ribonucleosides has been designed and synthesized. Two synthetic approaches to the key heterocyclic aglycon I, (i) a six-step classical heterocyclization starting from 5-chloro-1-methyl-4-nitropyrazole and (ii) a three-step cross-coupling and cyclization approach starting from the zinc 4,6-dichloropyrimidine, gave comparable total yield of 18% vs. 13%. The glycosylation of I was attempted by three different methods but only the Vorbruggen silyl-base protocol was efficient and stereoselective to give desired β-anomeric nucleoside intermediate. Its nucleophilic substitutions or cross-coupling reactions at position 8 and deprotection of the sugar moiety gave eight derivatives of pyrazolo-fused deazapurine ribonucleosides, e.g. II, some of which were weakly fluorescent. Me, amino and methylsulfanyl derivatives exerted sub-micromolar cytotoxic effects in vitro against a panel of cancer and leukemia cell lines, as well as antiviral effect against hepatitis C virus in the replicon assay.

Safety of 4-Nitro-1H-pyrazole, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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