Tag: 0-100

On March 11, 2015, Morrison, Angus; Carswell, Emma; Armer, Richard; Pesnot, Thomas; Bingham, Matilda; Bhamra, Inder; Kirkham, James; Colbon, Paul; Avery, Craig; McCarroll, Andrew; Testar, Richard published a patent.Category: pyrazoles-derivatives The title of the patent was Preparation of triazole derivatives as inhibitors of Raf kinases. And the patent contained the following:

Triazolyl compounds of formula [I; A = a 5-membered heterocyclic moiety; B = C6-14 aryl or C5-14 heteroaryl; L = ·SO 2 NRa , where Ra = H, C1-4 alkyl or C1-4 haloalkyl; R1 = C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C3-14 carbocyclyl or C3-14 heterocyclyl, each optionally substituted with 1-5 substituents selected from halo, ORb , SRb , NRbRc, NO, oxo, cyano, C1-4 acyl, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C(O)Rb and C(O)ORb ; R2 = H, halo, C1-4 alkyl or C1-4 haloalkyl; R3 = H, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, or C3-8 heterocycloalkyl; R4 = H, halo, OR5 , SR5 , NR5R6, NO, oxo, cyano, acyl, C(O)ORb , C(O)NRbRc , C1-6 alkyl, C3-14 carbocyclyl or C3·14 heterocyclyl; R5 and R6 are H, C(O)Rb, C1-4 alkyl, C1-4 haloalkyl, C3-8 carbocyclyl or C3-8 heterocyclyl; Rb, Rc = H, C1-4 alkyl, C1-4 haloalkyl, C1-4 acyl, C3-7 cycloalkyl or C3-7 halocycloalkyl; m = 0-3; n = 0-2] are prepared These compounds may be useful as inhibitors of Raf kinases, e.g. B-Raf and C-Raf. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Raf kinases, for example cancer, including lymphoma, leukemia and melanoma. Thus, N-[3-(5-bromo-2-tert-butyltriazol-4-yl)-2-fluorophenyl]-2,5-difluorobenzenesulfonamide was coupled with a mixture of 3-methoxy-1-tetrahydropyran-2-yl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole and 5-methoxy-1-tetrahydropyran-2-yl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole in the presence of tripotassium phosphate, tricyclohexylphosphine, and tris(dibenzylideneacetone)dipalladium(0) in DMF and water under heating in a microwave at 130° for 3 h to give N-[3-[2-tert-butyl-5-(3-methoxy-1-tetrahydropyran-2-ylpyrazol-4-yl)triazol-4-yl]-2-fluorophenyl]-2,5-difluorobenzenesulfonamide and N-[3-[2-tert-butyl-5-(5-methoxy-1-tetrahydropyran-2-ylpyrazol-4-yl)triazol-4-yl]-2-fluorophenyl]-2,5-difluorobenzenesulfonamide as an inseparable mixture which was stirred p-toluenesulfonic acid monohydrate in methanol for a total of 72 h to give N-[3-[2-tert-butyl-5-(3-methoxy-1H-pyrazol-4-yl)triazol-4-yl]-2-fluorophenyl]-2,5-difluorobenzenesulfonamide (II). II showed IC50 of <15 nM against B-Raf and C-Raf kinase, resp. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Category: pyrazoles-derivatives

The Article related to triazole preparation inhibitor raf kinase, pyrazolyltriazolylphenylbenzenesulfonamide preparation inhibitor raf kinase, cancer lymphoma leukemia melanoma treatment triazole preparation and other aspects.Category: pyrazoles-derivatives

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

On August 5, 2021, Wilson, Kevin J.; Schiller, Shawn E.R.; Negretti, Solymar published a patent.Related Products of 215610-30-3 The title of the patent was Carboxamide compounds for the treatment of BAF complex-related diseases and their preparation. And the patent contained the following:

The disclosure features compounds of formula I useful for the treatment of BAF complex-related disorders. Compounds of formula I wherein A is substituted oxetan-3-ylphenyl, (un)substituted bicyclic heterocyclic ring system; B is (un)substituted 6-membered heteroarylene and (un)substituted 9- to 10-membered bicyclic heteroarylene; L is a covalent bond, (un)substituted C1-3 alkylene, C2 alkynylene, (un)substituted C2 alkenylene, etc.; E is (un)substituted 3- to 10-membered cycloalkylene, (un)substituted 6- to 10-membered aryl, (un)substituted 5- to 10-membered heteroaryl, etc.; M is absent, (CR2R3)1-3; R1 is H and (un)substituted C1-6 alkyl; R2 and R3 are independently H, (un)substituted C1-6 alkyl and (un)substituted C1-6 heteroalkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cross-coupling of tert-Bu N-[(4-bromo-2-pyridyl)methyl]carbamate with Me 3-ethynylbenzoate; the resulting Me 3-[2-[2-[(tert-butoxycarbonylamino)methyl]-4-pyridyl]ethynyl]benzoate underwent hydrolysis to give Me 3-[2-[2-(aminomethyl)-4-pyridyl]ethynyl]benzoate, which underwent N-acylation with (4R)-4-cyano-4-methyl-chromane-6-carboxylic acid to give compound II. The invention compounds were evaluated for BRM and BRG1 inhibitory activity (some data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Related Products of 215610-30-3

The Article related to carboxamide preparation treatment baf complex disease, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Related Products of 215610-30-3

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

Kikalishvili, T. Dzh.; Kereselidze, Dzh. A. published an article in 2002, the title of the article was Quantum-chemical study of some physico-chemical properties of derivatives of pyrazole.COA of Formula: C4H6N2O And the article contains the following content:

By modern semiempirical quantum-chem. method the charges on the atoms, dipole moments, and ionization potentials of derivatives of pyrazole were calculated and the correlation anal. using Taft’s substituent constants was carried out. The possibility of quant. description of reactivity of pyrazoles was shown. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).COA of Formula: C4H6N2O

The Article related to pyrazole derivative structure property reactivity, Physical Organic Chemistry: Theoretical Organic Chemical Concepts, Including Quantum and Molecular Mechanical Studies and other aspects.COA of Formula: C4H6N2O

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

On April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Category: pyrazoles-derivatives The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Category: pyrazoles-derivatives

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazoles-derivatives

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

On April 1, 2021, Richards, Nicole; Lewis, Richard; Hamilton, Matthew; Ray, William; Alvarez, Fernando; Pfaffinger, Dana; Reyna, Naphtali; Cross, Jason; Ramaswamy, Suyambu Kesava Vijayan; Bardenhagen, Jennifer; Lightfoot, Yaima Luzardo; Acton, Paul; Goodwani, Sunil published a patent.Reference of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of 1-[(4,5-dihydro-1H-pyrazol-1-yl)carbonyl]bicyclo[1.1.1]pentane derivatives as inhibitors of receptor interacting protein kinase for the treatment of disease. And the patent contained the following:

The is invention is related to the preparation of compounds I [X = a bond, carbamoyl, carbonyl, (un)substituted alkylene; R1a, R1b = independently H, (un)substituted alkyl; or R1aNR1b= (un)substituted heterocycloalkyl or heteroaryl; R2 = H, OH, CN, halo, NH2, etc.] or salts thereof which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer. Thus, Wittig reaction between 3,5-difluorobenzaldehyde and 2-(triphenylphosphoranylidene)acetaldehyde, cyclization of (E)-3-(3,5-difluorophenyl)-2-propenal with NH2NH2 and reaction of 5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole with 3-(methoxycarbonyl)bicyclo[1.1.1]pentane-1-carboxylic acid gave II. Exemplified compounds I were tested for their RIPK1 activity (data given for representative compounds I). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Reference of 5-Methoxy-1H-pyrazole

The Article related to dihydropyrazolylcarbonylbicyclopentane derivative preparation receptor interacting protein kinase 1 inhibitor, ripk1 inhibitor dihydropyrazolylcarbonylbicyclopentane derivative preparation antiinflammatory anticancer neurodegenerative disorder and other aspects.Reference of 5-Methoxy-1H-pyrazole

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

《Direct electrochemical hydrodefluorination of trifluoromethyl ketones enabled by non-protic conditions》 was published in Chemical Science in 2021. These research results belong to Box, John R.; Atkins, Alexander P.; Lennox, Alastair J. J.. Name: 1-Methylpyrazole The article mentions the following:

CF2H groups are unique due to the combination of their lipophilic and hydrogen bonding properties. The strength of H-bonding is determined by the group to which it is appended. Several functional groups have been explored in this context including O, S, SO and SO2 to tune the intermol. interaction. Difluoromethyl ketones are under-studied in this context, without a broadly accessible method for their preparation Herein, authors describe the development of an electrochem. hydrodefluorination of readily accessible trifluoromethyl ketones. The single-step reaction at deeply reductive potentials is uniquely amenable to challenging electron-rich substrates and reductively sensitive functionality. Key to this success is the use of non-protic conditions enabled by an ammonium salt that serves as a reductively stable, masked proton source. Anal. of their H-bonding has revealed difluoromethyl ketones to be potentially highly useful dual H-bond donor/acceptor moieties. The results came from multiple reactions, including the reaction of 1-Methylpyrazole(cas: 930-36-9Name: 1-Methylpyrazole)

1-Methylpyrazole(cas: 930-36-9) 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: 1-Methylpyrazole

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

Britton, Luke; Skrodzki, Maciej; Nichol, Gary S.; Dominey, Andrew P.; Pawluc, Piotr; Docherty, Jamie H.; Thomas, Stephen P. published an article in ACS Catalysis. The title of the article was 《Manganese-Catalyzed C(sp2)-H Borylation of Furan and Thiophene Derivatives》.Quality Control of 1-Methylpyrazole The author mentioned the following in the article:

Aryl boronic esters are bench-stable, platform building-blocks that can be accessed through metal-catalyzed aryl C(sp2)-H borylation reactions. C(sp2)-H bond functionalization reactions using rare- and precious-metal catalysts are well established, and while examples using Earth-abundant alternatives have emerged, Mn catalysis remains lacking. The Mn-catalyzed C-H borylation of furan and thiophene derivatives is reported alongside an in situ activation method providing facile access to the active Mn hydride species. Mechanistic studies showed that blue light irradiation directly affected catalysis by action at the metal center, that C(sp2)-H bond borylation occurs through a C-H metalation pathway, and that the reversible coordination of pinacolborane to the catalyst gave a Mn borohydride complex, which was as an off-cycle resting state. The results came from multiple reactions, including the reaction of 1-Methylpyrazole(cas: 930-36-9Quality Control of 1-Methylpyrazole)

1-Methylpyrazole(cas: 930-36-9) 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. Quality Control of 1-Methylpyrazole

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

Category: pyrazoles-derivativesOn October 16, 2020 ,《Stereodivergent Synthesis of Alkenylpyridines via Pd/Cu Catalyzed C-H Alkenylation of Pyridinium Salts with Alkynes》 was published in Organic Letters. The article was written by Li, Wenjing; Tang, Juan; Li, Shun; Zheng, Xueli; Yuan, Maolin; Xu, Bin; Jiang, Weidong; Haiyan Fu; Li, Ruixiang; Chen, Hua. The article contains the following contents:

The first Pd/Cu catalyzed selective C2-alkenylation of pyridines with internal alkynes has been developed via the pyridinium salt activation strategy. Importantly, the configuration of the product alkenylpyridines could be tuned by the choice of the proper N-alkyl group of the pyridinium salts, thus allowing for both the Z- and E-alkenylpyridines synthesized with good regio- and stereoselectivity. A plausible mechanism was proposed based on the Hammett study and KIE experiment In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Category: pyrazoles-derivatives) was used in this study.

1-Methylpyrazole(cas: 930-36-9) 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. Category: pyrazoles-derivatives

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

《Highly active hybrid mesoporous silica-supported base organocatalysts for C-C bond formation》 was written by Erigoni, A.; Hernandez-Soto, M. C.; Rey, F.; Segarra, C.; Diaz, U.. Recommanded Product: 930-36-9 And the article was included in Catalysis Today on April 1 ,2020. The article conveys some information:

New base hybrid catalysts, based on silyl-derivatives of mols. carrying amino, diamino, pyrrolidine, pyrazolium and imidazolium functionalities were successfully achieved through post synthetic grafting onto M41S-type support. Different characterization techniques were implemented to study the characteristics of the materials, such as elemental anal., solid state MAS NMR and FTIR spectroscopies, X-ray diffraction (XRD), thermogravimetric and differential thermal analyses (TGA-DTA) and textural properties through N2 physisorption anal. The catalytic activity and recyclability of these compounds as base catalysts was demonstrated for C-C bond forming reactions such as Knoevenagel condensations and Michael additions rationalizing the differences observed as function of the reaction mechanisms. An enamine mechanism was proposed for Knoevenagel condensations and an enolate mechanism for Michael additions The experimental process involved the reaction of 1-Methylpyrazole(cas: 930-36-9Recommanded Product: 930-36-9)

1-Methylpyrazole(cas: 930-36-9) 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: 930-36-9

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

Li, Guangbin; Field, James A.; Zeng, Chao; Madeira, Camila Leite; Nguyen, Chi Huynh; Jog, Kalyani Vikas; Speed, David; Sierra-Alvarez, Reyes published their research in Chemosphere on February 29 ,2020. The article was titled 《Diazole and triazole inhibition of nitrification process in return activated sludge》.Category: pyrazoles-derivatives The article contains the following contents:

Azoles are emerging contaminants that are resistant to biodegradation during wastewater treatment. Their presence has been widely reported in wastewater effluents and receiving waters. In this work, the potential inhibition of nitrification process by six different azole compounds in wastewater treatment plants was investigated in batch bioassays. The azoles studied included three diazoles: pyrazole (Pz); 1-methylpyrazole (MePz); 3,5-dimethylpyrazole (DMePz); and three triazoles: 1,2,4-triazole (Tz); benzotriazole (BTz); and 5-Me benzotriazole (MeBTz). The concentration of azoles causing 50% inhibition (IC50) increased (azoles became less inhibitory) in the following order (mg L-1): BTz (1.99) < MeBTz (2.18) < Pz (2.69) < Tz (3.53) < DMePz (17.3) < MePz (49.6). No clear structure-inhibitory relationships were found using Log P and pKa as structural properties. The toxicity of any given azole may be related to the role of substituent groups on disabling/enabling binding to the active sites of metallo-enzymes in nitrifying microorganisms. This is exemplified by the low toxicity of MePz, which has a cyclic N blocked by a Me group. The observed inhibition caused to nitrifying bacteria is more severe than their cytotoxicity to other target organisms (e.g., methanogens and heterotrophic bacteria), suggesting a specific inhibition to the copper-containing enzyme, ammonium monooxygenase, in ammonia oxidizing nitrifying microorganisms. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpyrazole(cas: 930-36-9Category: pyrazoles-derivatives)

1-Methylpyrazole(cas: 930-36-9) 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. Category: pyrazoles-derivatives

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