Tag: 100-200

Safety of Methyl 1H-pyrazole-3-carboxylateIn 2011 ,《Esterification of pyrazole-3- and 4-carboxylic acids》 appeared in Russian Journal of General Chemistry. The author of the article were Saakyan, A. A.. The article conveys some information:

The esterification of pyrazole-3- and 4-carboxylic acids with MeOH was described.Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Safety of Methyl 1H-pyrazole-3-carboxylate) was used in this study.

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.Safety of Methyl 1H-pyrazole-3-carboxylate

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

Formula: C4H3F3N2In 2012 ,《Diversification of pyrazoles by microwave-assisted ligand free copper catalyzed N-arylation》 appeared in Bulletin of the Korean Chemical Society. The author of the article were Suh, Jeehee; Kang, Hee Sung; Kim, Ji-Eun; Yum, Eul Kgun. The article conveys some information:

Simple and efficient N-arylation of pyrazoles was achieved using microwave-assisted catalytic Cu reactions without organic ligands and with short reaction times. The N-arylation of pyrazole could be extended to various substituted pyrazoles and aryl halides. Yields of N-arylpyrazoles were highly dependent on the steric and electronic effects of the pyrazole substituents. Further functionalization of N-arylated iodopyrazoles in Cu- and Pd-catalyzed coupling reactions exhibited promising results for the diversification of pyrazoles. In the experiment, the researchers 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

In 1977,Gilman, Norman W.; Holland, Betty C.; Walsh, Gregory R.; Fryer, R. Ian published 《Nucleophilic displacement of aromatic fluorine. Part V. Use of nitrogen heterocycles as nucleophiles》.Journal of Heterocyclic Chemistry published the findings.Recommanded Product: 15366-34-4 The information in the text is summarized as follows:

I (R = F) reacted with imidazole, 2-methylimidazole, 3,5-bis(acetoxymethyl)pyrazole, pyrrole, di-Et 2-methyl-4,5-imidazoledicarboxylate, Me pyrrole-2-carboxylate, di-Me pyrazole-3,5-dicarboxylate, and Me pyrazole-3-carboxylate to give N-aryl heterocycles, e.g., II. In some cases the analogous reaction with I (R = Cl) failed to occur. Some substitution reactions of other aromatic fluorides were also examined The results came from multiple reactions, including the reaction of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Recommanded Product: 15366-34-4)

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.Recommanded Product: 15366-34-4

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

Kwiatkowski, Jacek; Liu, Boping; Pang, Shermaine; Binte Ahmad, Nur Huda; Wang, Gang; Poulsen, Anders; Yang, Haiyan; Poh, Yong Rui; Tee, Doris Hui Ying; Ong, Esther; Retna, Priya; Dinie, Nurul; Kwek, Perlyn; Wee, John Liang Kuan; Manoharan, Vithya; Low, Choon Bing; Seah, Peck Gee; Pendharkar, Vishal; Sangthongpitag, Kanda; Joy, Joma; Baburajendran, Nithya; Jansson, Anna Elisabet; Nacro, Kassoum; Hill, Jeffrey; Keller, Thomas H.; Hung, Alvin W. published an article on January 23 ,2020. The article was titled 《Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2》, and you may find the article in Journal of Medicinal Chemistry.Quality Control of 4-Bromo-5-cyclopropyl-1H-pyrazole The information in the text is summarized as follows:

Dysregulation of translation initiation factor 4E (eIF4E) activity occurs in various cancers. Mitogen-activated protein kinase (MAPK) interacting kinases 1 and 2 (MNK1 and MNK2) play a fundamental role in activation of eIF4E. Structure-activity relationship-driven expansion of a fragment hit led to discovery of dual MNK1 and MNK2 inhibitors based on a novel pyridine-benzamide scaffold. The compounds possess promising in vitro and in vivo pharmacokinetic profiles and show potent on target inhibition of eIF4E phosphorylation in cells. In the experiment, the researchers used 4-Bromo-5-cyclopropyl-1H-pyrazole(cas: 957345-28-7Quality Control of 4-Bromo-5-cyclopropyl-1H-pyrazole)

4-Bromo-5-cyclopropyl-1H-pyrazole(cas: 957345-28-7) 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. Quality Control of 4-Bromo-5-cyclopropyl-1H-pyrazole

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

Name: Methyl 1H-pyrazole-3-carboxylateIn 2021 ,《Route Design to Manufacture: Synthesis of the Heterocyclic Fragment of AZD5718 Using a Non-cryogenic Lithiation-Alkoxycarbonylation Reaction》 was published in Organic Process Research & Development. The article was written by Burns, Matthew; Perkins, Dave; Chan, Lai C.; Pilling, Michael J.; Jawor-Baczynska, Anna; Mullen, Alexander K.; Steven, Alan; Wimsey, Chris; Elmekawy, Ahmed; Lamacraft, Alex; Dobson, Benjamin C.; McMillan, Angus E.; Hose, David R. J.; Inglesby, Phillip A.; Raw, Steven A.; Jones, Martin F.. The article contains the following contents:

Route design and process development of the small nitrogen heterocycle I, a constituent of AZD5718 (II), is described. The novel synthetic sequence to I involves a desymmetrizing alkylation of 4-nitropyrazole, a non-cryogenic lithiation-alkoxycarbonylation, and a global reduction-cyclization. This new synthetic route was implemented in the manufacture of I and was able to deliver over 1000 kg of product with a yield of 77% over the three stages. In the experiment, the researchers used many compounds, for example, 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

Computed Properties of C5H6N2O2In 1976 ,《Unusual reaction of 3-carbomethoxy-Δ2-pyrazoline in the presence of lead tetraacetate》 appeared in Khimiya Geterotsiklicheskikh Soedinenii. The author of the article were Akhrem, A. A.; Kvasyuk, E. I.; Mikhailopulo, I. A.. The article conveys some information:

Treatment of pyrazolinecarboxylate I with Pb(OAc)4 in dry C6H6 30 min at 70° gave 71% II and 14% III whose structures were confirmed by ir, uv, and NMR spectra. In the experiment, the researchers used many compounds, for example, Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Computed Properties of 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.Computed Properties of C5H6N2O2

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

The author of 《Inhibition of fatty acid release by pyrazole derivatives》 were Bizzi, Adalgisa. And the article was published in Progress in Biochemical Pharmacology in 1968. Recommanded Product: (3-methyl-1H-pyrazol-5-yl)methanol The author mentioned the following in the article:

In rats, 3,5-dimethylpyrazole (I) is quiet active in decreasing free fatty acid (FFA) and glycerol in adipose tissue as well as in plasma with doses as low as 50 μg/kg, i.p. In plasma after 2 hr, I and 5-carboxyl-3-methylpyrazole (II) appear more active than 3-methylpyrazole. When tested in vitro on the release of FFA from adipose tissue, II appeared to be the most active. The 3 compounds when given orally in doses of 0.75-30 mg/kg also produce up to a 50% decrease in plasma triglycerides. This effect is proportional to the dose used. The experimental part of the paper was very detailed, including the reaction process of (3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7Recommanded Product: (3-methyl-1H-pyrazol-5-yl)methanol)

(3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7) 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. Recommanded Product: (3-methyl-1H-pyrazol-5-yl)methanol

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

In 2016,Yu, Haibo; Cheng, Yan; Xu, Man; Song, Yuquan; Luo, Yanmei; Li, Bin published 《Synthesis, Acaricidal Activity, and Structure-Activity Relationships of Pyrazolyl Acrylonitrile Derivatives》.Journal of Agricultural and Food Chemistry published the findings.Reference of Methyl 1H-pyrazole-3-carboxylate The information in the text is summarized as follows:

A series of novel pyrazolyl acrylonitrile derivatives were designed, targeting Tetranychus cinnabarinus, and synthesized. Their structures were identified by combination of 1H NMR, 13C NMR and MS spectra. The structures of compounds (I) and (II) were further confirmed by X-ray diffraction. Extensive greenhouse bioassays indicated that compound II exhibits excellent acaricidal activity against all developmental stages of Tetranychus cinnabarinus, which is better than the commercialized compounds cyenopyrafen and spirodiclofen. It was shown that the acute toxicity of compounds II to mammals is quite low. The structure-activity relationships are also discussed. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Reference of Methyl 1H-pyrazole-3-carboxylate)

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.Reference of Methyl 1H-pyrazole-3-carboxylate

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

In 2012,Wu, Yuchuan; Li, Jianchang; Wu, Junjun; Morgan, Paul; Xu, Xin; Rancati, Fabio; Vallese, Stefania; Raveglia, Luca; Hotchandani, Rajeev; Fuller, Nathan; Bard, Joel; Cunningham, Kristina; Fish, Susan; Krykbaev, Rustem; Tam, Steve; Goldman, Samuel J.; Williams, Cara; Mansour, Tarek S.; Saiah, Eddine; Sypek, Joseph; Li, Wei published 《Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD)》.Bioorganic & Medicinal Chemistry Letters published the findings.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

Chronic obstructive pulmonary disease (COPD) is an inflammatory lung disease associated with irreversible progressive airflow limitation. Matrix metalloproteinase-12 (MMP-12) has been characterized to be one of the major proteolytic enzymes to induce airway remodeling, destruction of elastin and the aberrant remodeling of damaged alveoli in COPD and asthma. The goal of this project is to develop and identify an orally potent and selective small mol. inhibitor of MMP-12 for treatment of COPD and asthma. Syntheses and structure-activity relationship (SAR) studies of a series of dibenzofuran (DBF) sulfonamides as MMP-12 inhibitors are described. Potent inhibitors of MMP-12 with excellent selectivity against other MMPs were identified. Compound I (MMP118), which exhibits excellent oral efficacy in the MMP-12 induced ear-swelling inflammation and lung inflammation mouse models, had been successfully advanced into Development Track status.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole) 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: 3-(Trifluoromethyl)-1H-pyrazole

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

In 2010,Kabir, M. Shahjahan; Namjoshi, Ojas A.; Verma, Ranjit; Polanowski, Rebecca; Krueger, Sarah M.; Sherman, David; Rott, Marc A.; Schwan, William R.; Monte, Aaron; Cook, James M. published 《A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives》.Bioorganic & Medicinal Chemistry published the findings.Name: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

Novel acrylic acid Et ester derivatives were synthesized and evaluated as potential agents against Mycobacterium species. A versatile and efficient copper-catalyzed coupling process was developed and used to prepare a library of substituted acrylic acid Et ester analogs. Min. inhibitory concentration assays indicated that two of these compounds 3 and 4 (I) have greater in vitro activity against Mycobacterium smegmatis than rifampin, one of the current, first-line anti-mycobacterial chemotherapeutic agents. Moreover, members of this new class of compounds appear to exhibit a specific anti-mycobacterial effect and do not inhibit the growth of the other Gram-pos. or Gram-neg. species tested. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Name: 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.Name: 3-(Trifluoromethyl)-1H-pyrazole

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