Category: 385-00-2

An article Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators WOS:000507987200002 published article about PROTEIN-PROTEIN INTERACTION; OXIDATIVE STRESS; DIMETHYL FUMARATE; KEAP1; INHIBITOR; DISCOVERY; BINDING in [Ma, Bin; Lucas, Brian; Capacci, Andrew; Lin, Edward Yin-Shiang; Jones, John Howard; Dechantsreiter, Michael; Enyedy, Istvan] Biogen, Med Chem, 225 Binney St, Cambridge, MA 02142 USA; [Marcotte, Douglas] Biogen, Biophys, 225 Binney St, Cambridge, MA 02142 USA; [Xiao, Guangqing] Biogen, Drug Metab & Pharmacokinet, 225 Binney St, Cambridge, MA 02142 USA; [Li, Bing; Richter, Karl] Biogen, Res & Early Dev, 225 Binney St, Cambridge, MA 02142 USA; [Lucas, Brian] Skyhawk Therapeut, Waltham, MA 02451 USA; [Xiao, Guangqing] Sunov Pharmaceut, Marlborough, MA 01752 USA in 2020, Cited 23. Recommanded Product: 2,6-Difluorobenzoic acid. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

Nrf2 is a transcription factor regulating expression of the Phase II Antioxidant Response and plays an important role in neuroprotection and detoxification. Nrf2 activation is inhibited by interaction with Keap1. Covalent Keap1 inhibitors such as dimethyl fumarate (DMF) and RTA-408 are either on the market or in late stage clinical trials which implies potential benefit of Nrf2 activation. Activation of Nrf2 by disrupting Nrf2-Keap1 interaction through a non-covalent small molecule is an attractive approach with the promise of greater selectivity. However, there are no known non-covalent Nrf2 activators with acceptable pharmacokinetic properties to test the hypothesis in vivo. Based on our early reported work, using structural-based design, followed by extensive SAR exploration, we have identified a novel series of non-covalent Nrf2 activators, with sub-nanomolar binding affinity on Keap1 and single digit nanomolar activity in an astrocyte assay. A representative analog shows excellent oral PK and good Nrf2-dependent gene inductions in kidney. These results provide a peripheral in vivo tool compound to validate the biology of non-covalent activation of Nrf2.

Recommanded Product: 2,6-Difluorobenzoic acid. Welcome to talk about 385-00-2, If you have any questions, you can contact Ma, B; Lucas, B; Capacci, A; Lin, EYS; Jones, JH; Dechantsreiter, M; Enyedy, I; Marcotte, D; Xiao, GQ; Li, B; Richter, K or send Email.

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Authors Sun, DL; Wang, YR; Zhang, QH; Pang, JX in PERGAMON-ELSEVIER SCIENCE LTD published article about TRANSFORMATION PRODUCTS; DEGRADATION-PRODUCTS; IDENTIFICATION; FOOD; MS; CHLORPYRIFOS; INSECTICIDE; PESTICIDES; POLLUTANTS; RESIDUES in [Sun, Dali; Zhang, Qinghai] Guizhou Med Univ, Coll Food Safety, Guiyang 550025, Guizhou, Peoples R China; [Pang, Junxiao] Guiyang Univ, Food & Pharmaceut Engn Inst, Key Lab Crit Technol Degradat Pesticide Residues, Guiyang 550005, Guizhou, Peoples R China; [Sun, Dali; Zhang, Qinghai] Guizhou Med Univ, Key Lab Environm Pollut Monitoring & Dis Control, Guiyang 550025, Guizhou, Peoples R China; [Wang, Yunru] Guangxi Subtrop Crops Res Inst, Nanning 530001, Peoples R China in 2019, Cited 30. SDS of cas: 385-00-2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

Etoxazole is a newly registered and widely used acaricide. However, its metabolites were not fully understood and might exhibit similar or even higher toxicity than parent compound. Therefore, in this study, the metabolites of etoxazole in citrus, soil and earthworms were firstly identified by an ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS). Four potential metabolites in citrus, 11 in soil, and 8 in earthworms were determined. These metabolites were then further structural elucidated based on the fragment pathways, and accurate mass measurement. The distributions of etoxazole and its main metabolites (M1, M2, M3, M4 and M5) which were identified as the dehydrogenation, hydrolysis, oxidation products of etoxazole (M0) were also monitored in citrus, soil and earthworms at different exposure periods. The 45 days exposure experiment showed that M0 gradually decreased in citrus and soil samples by 80% and 28% of the initial amounts, respectively. In earthworm samples, M0 accumulated in the bodies of the worms during 24 days exposure and then decreased with time. The dissipation rate of etoxazole were citrus > earthworms > soil. Concentrations of M1 and M3 in soil were found continuously increased with time during the experimental period. Moreover, the persistence of M1 in earthworm samples was also observed. Great attention should be paid to these two compounds due to their potential risks to both environmental and human health. (C) 2019 Published by Elsevier Ltd.

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Recommanded Product: 2,6-Difluorobenzoic acid. I found the field of Chemistry very interesting. Saw the article Gold Catalyzed Decarboxylative Cross-Coupling of Iodoarenes published in 2020, Reprint Addresses Topczewski, JJ (corresponding author), Univ Minnesota Twin Cities, Dept Chem, Minneapolis, MN 55455 USA.; Neufeldt, SR (corresponding author), Montana State Univ, Dept Chem & Biochem, Bozeman, MT 59717 USA.. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid.

This report details a decarboxylative cross-coupling of (hetero)aryl carboxylates with iodoarenes in the presence of a gold catalyst (>25 examples, up to 96% yield). This reaction is site specific, which overcomes prior limitations associated with gold catalyzed oxidative coupling reactions. The reactivity of the (hetero)aryl carboxylate correlates qualitatively to the field effect parameter (F-ortho). Reactions with isolated gold complexes and DFT calculations support a mechanism proceeding through oxidative addition at a gold(I) cation with decarboxylation being viable at either a gold(I) or a silver(I) species.

Recommanded Product: 2,6-Difluorobenzoic acid. Welcome to talk about 385-00-2, If you have any questions, you can contact Daley, RA; Morrenzin, AS; Neufeldt, SR; Topczewski, JJ or send Email.

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Quality Control of 2,6-Difluorobenzoic acid. Currie, I; Sleebs, BE in [Currie, Iain; Sleebs, Brad E.] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3052, Australia; [Currie, Iain; Sleebs, Brad E.] Univ Melbourne, Dept Med Biol, Parkville, Vic 3010, Australia published Synthesis of Acyl Phosphoramidates Employing a Modified Staudinger Reaction in 2021, Cited 24. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

A one-step synthesis of acyl phosphoramidates from a variety of functionalized acyl azides has been developed employing trimethylsilyl chloride as an activating agent in a modified Staudinger reaction. The methodology was further adapted to include the in situ generation of the acyl azides from a diverse selection of carboxylic acids and hydrazide starting synthons. The reaction scope was extended to include the synthesis of imidodiphosphates and the natural product Microcin C.

Quality Control of 2,6-Difluorobenzoic acid. Welcome to talk about 385-00-2, If you have any questions, you can contact Currie, I; Sleebs, BE or send Email.

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In 2020 J MED CHEM published article about CYSTEINE PROTEASE; ALDEHYDE INHIBITORS; IN-VITRO; BIOLOGICAL EVALUATION; ANTIVIRAL ACTIVITY; SARS-CORONAVIRUS; FORMAZAN ASSAY; DESIGN; AG7088; PAPAIN in [Hoffman, Robert L.; Kania, Robert S.; Brothers, Mary A.; Davies, Jay F.; Ferre, Rose A.; Gajiwala, Ketan S.; He, Mingying; Kozminski, Kirk; Li, Lilian Y.; Lockner, Jonathan W.; Lou, Jihong; Marra, Michelle T.; Mitchell, Lennert J., Jr.; Murray, Brion W.; Nieman, James A.; Noell, Stephen; Planken, Simon P.; Ryan, Kevin; Smith, George J., III; Solowiej, James E.; Steppan, Claire M.] Pfizer Worldwide Res & Dev, San Diego, CA 92121 USA; [Hogan, Robert J.; Rowe, Thomas; Taggart, Barbara] Southern Res Inst, Birmingham, AL 35205 USA in 2020, Cited 45. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. Application In Synthesis of 2,6-Difluorobenzoic acid

The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1 that caused severe acute respiratory syndrome (SARS) in 2002. Both SARS coronavirus genomes encode two overlapping large polyproteins, which are cleaved at specific sites by a 3C-like cysteine protease (3CL(pro)) in a post-translational processing step that is critical for coronavirus replication. The 3CL(pro) sequences for CoV-1 and CoV-2 viruses are 100% identical in the catalytic domain that carries out protein cleavage. A research effort that focused on the discovery of reversible and irreversible ketone-based inhibitors of SARS CoV-1 3CL(pro) employing ligand-protease structures solved by X-ray crystallography led to the identification of 3 and 4. Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CL(pro) with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

Application In Synthesis of 2,6-Difluorobenzoic acid. Welcome to talk about 385-00-2, If you have any questions, you can contact Hoffman, RL; Kania, RS; Brothers, MA; Davies, JF; Ferre, RA; Gajiwala, KS; He, MY; Hogan, RJ; Kozminski, K; Li, LLY; Lockner, JW; Lou, JH; Marra, MT; Mitchell, LJ; Murray, BW; Nieman, JA; Noell, S; Planken, SP; Rowe, T; Ryan, K; Smith, GJ; Solowiej, JE; Steppan, CM; Taggart, B or send Email.

Reference:
Isothiazole – Wikipedia,
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In 2019 CHEMOSPHERE published article about COLLOID TRANSPORT; SILVER NANOPARTICLES; ANAEROBIC BIOREMEDIATION; MINERALIZATION PATHWAYS; FLOW CONDITIONS; ORGANIC-MATTER; POROUS-MEDIA; HEAVY-METALS; MOBILIZATION; TRANSFORMATION in [Liang, Xiaolong; Radosevich, Mark; Loffler, Frank; Schaeffer, Sean M.; Zhuang, Jie] Univ Tennessee, Dept Biosyst Engn & Soil Sci, Knoxville, TN 37996 USA; [Loffler, Frank] Univ Tennessee, Dept Microbiol, Dept Civil & Environm Engn, Ctr Environm Biotechnol, Knoxville, TN 37996 USA; [Loffler, Frank] Oak Ridge Natl Lab, Biosci Div, Oak Ridge, TN 37831 USA in 2019, Cited 60. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. Formula: C7H4F2O2

In subsurface bioremediation, electron donor addition promotes microbial Fe(lII)-oxide mineral reduction that could change soil pore structure, release colloids, and alter soil surface properties. These processes in turn may impact bioremediation rates and the ultimate fate of contaminants. Columns packed with water-stable, Fe-oxide-rich soil aggregates were infused with acetate-containing artificial groundwater and operated for 20 d or 60 d inside an anoxic chamber. Soluble Fe(II) and soil colloids were detected in the effluent within one week after initiation of the acetate addition, demonstrating Fe(III)-bioreduction and colloid formation. Diffusible Br-, less diffusible 2,6-difluorobenzoate (DFBA), and non-diffusible silica-shelled silver nanoparticles (SSSNP) were used as tracers in transport experiments before and after the bioreduction. The transport of Br- was not influenced by the bioreduction. DFBA showed earlier breakthrough and less tailing after the bioreduction, suggesting alterations in flow paths and soil surface chemistry during the 20-d bioreduction treatment. Similarly, the bioreduction increased the transport of SSSNP very significantly, with mass recovery increasing from 1.7% to 25.1%. Unexpectedly, the SSSNP was completely retained in the columns when the acetate injection was extended from 20 to 60 d, while the mass recovery of DFBA decreased from 89.1% to 84.1% and Br showed no change. The large change in the transport of SSSNP was attributed to soil aggregate breakdown and colloid release (causing mechanical straining of SSSNP) and the exposure of iron oxide surfaces previously unavailable within aggregate interiors (facilitating attachment of SSSNP). These results suggest a time dependent fashion of microbial effect on the transport of diffusivity-varying tracers. (C) 2018 Elsevier Ltd. All rights reserved.

Welcome to talk about 385-00-2, If you have any questions, you can contact Liang, XL; Radosevich, M; Loffler, F; Schaeffer, SM; Zhuang, J or send Email.. Formula: C7H4F2O2

Reference:
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,Isothiazole – ScienceDirect.com

COA of Formula: C7H4F2O2. In 2021 EUR J ORG CHEM published article about ANTI-MARKOVNIKOV ADDITION; CARBOXYLIC-ACIDS; ENOL ESTERS; TERMINAL ALKYNES; CATALYZED ADDITION; GOLD(I)-CATALYZED ADDITION; STEREOSPECIFIC SYNTHESIS; RUTHENIUM COMPLEX; INTERNAL ALKYNES; VINYL ESTERS in [Kumari, Chandresh; Goswami, Avijit] Indian Inst Technol Ropar, Dept Chem, Nangal Rd, Rupnagar 140001, Punjab, India in 2021, Cited 96. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

We report an efficient and straight forward access to nitrile substituted enol esters via ionic liquid [BMIM]OH mediated hydrocarboxylation of alkynylnitriles under mild conditions. This atom economical transition metal-free protocol gives an easy access to a variety of such enol esters with excellent regio and Z-stereoselectivity. Reusability of [BMIM]OH without losing of significant amount of yield is another noticeable feature of this article.

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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

COA of Formula: C7H4F2O2. I found the field of Agriculture; Entomology very interesting. Saw the article Design, synthesis, and insecticidal activities of novel 5-substituted 4,5-dihydropyrazolo[1,5-a]quinazoline derivatives published in 2021, Reprint Addresses Zhao, C; Xu, HH (corresponding author), South China Agr Univ, Minist Educ, State Key Lab Conservat & Utilizat Subtrop Agrobi, Guangzhou 510642, Peoples R China.; Zhao, C; Xu, HH (corresponding author), South China Agr Univ, Minist Educ, Key Lab Nat Pesticide & Chem Biol, Guangzhou 510642, Peoples R China.. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid.

BACKGROUND: Chemical pesticides are the main measures for pest control, but have caused growing resistance of pests and brought a series of environmental problems. Development of high-efficient insecticidal molecules with novel scaffolds is therefore particularly urgent. RESULTS: Based on a [5 + 1] annulation reaction with 5-amino-1H-phenylpyrazole and dialkyl bromomalonate, 27 novel five-substituted 4,5-dihydropyrazolo[1,5-a]quinazolines were designed following the intermediate derivatization method and synthesized. Bioassay results indicated that most of the test compounds displayed good insecticidal activities against Plutella xylostella, Spodoptera frugiperda, and Solenopsis invicta. In particular, the insecticidal activities of compounds 4a, 4f, and 4m against P. xylostella [median lethal concentration (LC50) values ranged from 3.87 to 5.10 mg L-1] were comparable to that of indoxacarb (LC50 = 4.82 mg L-1). In addition, compounds 4a and 9e showed similar high insecticidal activities against Spodoptera frugiperda (mortality rate = 79.63% and 72.12%) at 100 mg L-1, comparable to that of fipronil (mortality rate: 68.44%); compound 9a showed possible delayed toxicity against Solenopsis invicta (mortality rate: 95.66%) after 5 days of treatment at 1.0 mg L-1. CONCLUSION: Due to their high insecticidal activities against P. xylostella, compound 4m, 4a, and 4f could be considered as qualified candidates for novel insecticide. Several other 4,5-dihydropyrazolo[1,5-a]quinazolines with relatively high bioactivity, such as compounds 9a and 9e, are also worth further optimization as potential insecticide or anticide candidates.

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Reference:
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Recommanded Product: 385-00-2. Authors Lin, TT; Li, JC; Liu, LP; Li, YQ; Jiang, HL; Chen, KX; Xu, P; Luo, C; Zhou, B in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about in [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 200031, Peoples R China; [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Xu, Pan; Luo, Cheng] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Chem Biol,Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Zhou, Bing] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng; Zhou, Bing] Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China in 2021, Cited 39. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

Cyclin-dependent kinases play significant roles in cell cycle progression and are promising targets for cancer therapy. However, most potent CDK inhibitors lack the balance between efficacy and safety because of poor selectivity. Given the roles of CDK2 in tumorigenesis, selective CDK2 inhibition may provide therapeutic benefits against certain cancer. In this study, a series of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives were designed, synthesized, and evaluated. The most selective compound DC-K2in212 in this series exhibited high potency towards CDK2 and had effective anti-proliferative activity against A2058 melanoma cell line and MV4-11 leukemia cell line while exhibiting low toxic effect on human normal cell lines MRC5 and LX2. The molecular modeling illustrated that compound DC-K2in212 had the similar binding mode with CDK2 as C-73, the most selective CDK2 inhibitor reported so far, which might account for selectivity against CDK2 over CDK1. Further biological studies revealed that compound DC-K2in212 suppressed CDK2-associated downstream signaling pathway, blocked cell cycle progression, and induced cellular apoptosis. Therefore, compound DC-K2in212 could serve as a potential CDK2 inhibitor for further development. (c) 2021 Elsevier Masson SAS. All rights reserved.

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In 2021 ANGEW CHEM INT EDIT published article about VISIBLE-LIGHT PHOTOREDOX; CROSS-COUPLING REACTIONS; ORGANIC AZIDES; CURTIUS REARRANGEMENT; PROTECTED AMINES; CARBOXYLIC-ACIDS; H AMINATION; CHEMISTRY; MILD; DIVERSITY in [Zhang, Yipin; Ge, Xia; Lu, Hongjian; Li, Guigen] Nanjing Univ, Sch Chem & Chem Engn, Jiangsu Key Lab Adv Organ Mat, Inst Chem & Biomed Sci, Nanjing 210093, Peoples R China; [Li, Guigen] Texas Tech Univ, Dept Chem & Biochem, Lubbock, TX 79409 USA in 2021, Cited 80. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2. Recommanded Product: 2,6-Difluorobenzoic acid

Transition-metal-catalyzed sp(2) C-N bond formation is a reliable method for the synthesis of aryl amines. Catalytic sp(3) C-N formation reactions have been reported occasionally, and methods that can realize both sp(2) and sp(3) C-N formation are relatively unexplored. Herein, we address this challenge with a method of catalytic decarboxylative C-N formation that proceeds through a cascade carboxylic acid activation, acyl azide formation, Curtius rearrangement and nucleophilic addition reaction. The reaction uses naturally abundant organic carboxylic acids as carbon sources, readily prepared azidoformates as the nitrogen sources, and 4-dimethylaminopyridine (DMAP) and Cu(OAc)(2) as catalysts with as low as 0.1 mol % loading, providing protected alkyl, alkenyl and aryl amines in high yields with gaseous N-2 and CO2 as the only byproducts. Examples are demonstrated of the late-stage functionalization of natural products and drug molecules, stereospecific synthesis of useful alpha-chiral alkyl amines, and rapid construction of different ureas and primary amines.

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Reference:
Isothiazole – Wikipedia,
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