Tag: 200-300

The author of 《Intramolecular Cyclization of Vinyldiazoacetates as a Versatile Route to Substituted Pyrazoles》 were Drikermann, Denis; Kerndl, Valerie; Goerls, Helmar; Vilotijevic, Ivan. And the article was published in Synlett in . Category: pyrazoles-derivatives The author mentioned the following in the article:

Vinyldiazo compounds undergo a thermal electrocyclization to form pyrazoles in yields of up to 95%. The reactions are operationally simple, use readily available starting materials, require no intervention of a catalyst, and enable the synthesis of mono-, di- and tri-substituted pyrazoles. With the ability to produce highly substituted pyrazoles and the flexibility in installing various types of substituents, this method constitutes a new entry to this valuable heterocyclic scaffold and may be of interest to all branches of the chem. industry. In addition to this study using Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate, there are many other studies that have used Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8Category: pyrazoles-derivatives) was used in this study.

Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8) 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. Category: pyrazoles-derivatives

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

In 2014,Sharp, Phillip P.; Garnier, Jean-Marc; Huang, David C. S.; Burns, Christopher J. published 《Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition》.MedChemComm published the findings.Related Products of 847818-74-0 The information in the text is summarized as follows:

The ability of various functional groups to engage the acetyl-lysine (KAc) binding site within bromo- and extra-terminal domain (BET) protein family members BRD2, BRD3 and BRD4 was evaluated by screening small mol. fragments – coupled to a known arylsulfonamide scaffold – in biochem. inhibition assays. Useful structure activity relationships have been established and novel functional groups that bind to the KAc binding pocket identified. Addnl. microsomal degradation studies were also undertaken revealing significant differences in metabolic stability between two commonly employed BET inhibitor fragments. 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: 847818-74-0Related Products of 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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Related Products of 847818-74-0

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

《DMSO-catalysed late-stage chlorination of (hetero)arenes》 was published in Nature Catalysis in 2020. These research results belong to Song, Song; Li, Xinyao; Wei, Jialiang; Wang, Weijin; Zhang, Yiqun; Ai, Lingsheng; Zhu, Yuchao; Shi, Xiaomeng; Zhang, Xiaohui; Jiao, Ning. Category: pyrazoles-derivatives The article mentions the following:

A highly efficient aromatic chlorination of arenes such as 1-methyl-indazole, imidazo[1,2-a]pyrazine, phenylthiophene, anthracene, etc. that is catalyzed by DMSO with N-chlorosuccinimide as the chloro source is reported. The mild conditions, easy-availability and stability of the catalyst and reagents, as well as good functional-group tolerance, showed the approach to be a versatile protocol for the late-stage aromatic chlorination of complex natural products, e.g., papaverine, drugs, e.g., diclofenac and peptides, e.g., I. The multi-gram experiment and low-cost of N-chlorosuccinimide and DMSO show great potential for drug discovery and development in industrial applications. 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: 847818-74-0Category: pyrazoles-derivatives)

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. Category: pyrazoles-derivatives

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

In 2017,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published 《Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4》.MedChemComm published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:

The replacement of acylamino group by cyclic substituents in the position 4 of the pyrazolo[3,4-d]pyrimidine scaffold I [R = Ph, pyridin-3-yl, 1-methyl-1H-pyrazol-5-yl, etc.], led to highly active sigma-1 receptor (σ1R) ligands. Ph or pyrazolyl groups were the best in terms of affinity for the σ1R and the compound I [R = 1-methyl-1H-pyrazol-5-yl], was the most selective. Compound I [R = 1-methyl-1H-pyrazol-5-yl] was also one of the best σ1R ligands ever described in terms of lipophilic ligand efficiency, which translated into a good physicochem. and ADMET profile. In addition, compound I [R = 1-methyl-1H-pyrazol-5-yl] was identified as an antagonist of the σ1R in view of its potent antinociceptive profile in several pain models in mice.1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole) 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. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2018 ,《A robust iron catalyst for the selective hydrogenation of substituted (iso)quinolones》 was published in Chemical Science. The article was written by Sahoo, Basudev; Kreyenschulte, Carsten; Agostini, Giovanni; Lund, Henrik; Bachmann, Stephan; Scalone, Michelangelo; Junge, Kathrin; Beller, Matthias. The article contains the following contents:

By applying N-doped carbon modified iron-based catalysts, the controlled hydrogenation of N-heteroarenes, especially (iso)quinolines, is achieved. The catalysts are prepared by pyrolysis of a carbon-impregnated composite, obtained from iron(II) acetate and N-aryliminopyridines. As demonstrated by TEM, XRD, XPS and Raman spectroscopy, the synthesized material is composed of Fe(0), Fe3C and FeNx in a N-doped carbon matrix. The decent catalytic activity of this robust and easily recyclable Fe-material allowed for the selective hydrogenation of various (iso)quinoline derivatives, even in the presence of reducible functional groups, such as nitriles, halogens, esters and amides. For a proof-of-concept, this nanostructured catalyst was implemented in the multistep synthesis of natural products and pharmaceutical lead compounds as well as modification of photoluminescent materials. As such this methodol. constitutes the first heterogeneous iron-catalyzed hydrogenation of substituted (iso)quinolines with synthetic importance. After reading the article, we found that the author used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 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. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

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

《Correction to “”Modular, Step-Efficient Palladium-Catalyzed Cross-Coupling Strategy To Access C6-Heteroaryl 2-Aminopurine Ribonucleosides”” [Erratum to document cited in CA167:176274]》 was written by Buchanan, Helena S.; Pauff, Steven M.; Kosmidis, Tilemachos D.; Taladriz-Sender, Andrea; Rutherford, Olivia I.; Hatit, Marine Z. C.; Fenner, Sabine; Watson, Allan J. B.; Burley, Glenn A.. Related Products of 847818-74-0This research focused ontriazole isoxazole isonitrile nucleoside preparation cycloaddition erratum; aminopurine nucleoside chloroguanosine Suzuki Miyaura chloroguanosine heteroarylaminopurine Sonogashira coupling; palladium catalyzed coupling heteroaryl aminopurine nucleoside cycloaddition isonitrile isoxazole; erratum. The article conveys some information:

The following statement was inadvertently omitted from the Acknowledgments section of the manuscript: “”This work was supported by an EPSRC-GSK industrial CASE studentship for H.S.B. 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: 847818-74-0Related Products of 847818-74-0)

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. Related Products of 847818-74-0

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

The author of 《Rapid Identification of Novel Allosteric PRC2 Inhibitors》 were Read, Jon A.; Tart, Jonathan; Rawlins, Philip B.; Gregson, Clare; Jones, Karen; Gao, Ning; Zhu, Xiahui; Tomlinson, Ron; Code, Erin; Cheung, Tony; Chen, Huawei; Kawatkar, Sameer P.; Bloecher, Andy; Bagal, Sharan; O’Donovan, Daniel H.; Robinson, James. And the article was published in ACS Chemical Biology in 2019. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The author mentioned the following in the article:

Enhancer of zeste homolog 2 (EZH2), the catalytic subunit of polycomb repressive complex 2 (PRC2), regulates chromatin state and gene expression by methylating histone H3 lysine 27. EZH2 is overexpressed or mutated in various hematol. malignancies and solid cancers. Our previous efforts to identify inhibitors of PRC2 methyltransferase activity by high-throughput screening (HTS) resulted in large numbers of false positives and thus a significant hit deconvolution challenge. More recently, others have reported compounds that bind to another PRC2 core subunit, EED, and allosterically inhibit EZH2 activity. This mechanism is particularly appealing as it appears to retain potency in cell lines that have acquired resistance to ortho steric EZH2 inhibition. By designing a fluorescence polarization probe based on the reported EED binding compounds, we were able to quickly and cleanly re-triage our previously challenging HTS hit list and identify novel allosteric PRC2 inhibitors. The experimental process involved the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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