Category: 162046-61-9

Zhou, Guanyu; Huang, Zhibin; Xu, Xu; Fang, Zhang; Huang, Pengcheng; Deng, Zefeng; Li, Bao; Zhao, Yingsheng published the artcile< Rhodium(III)-Catalyzed Synthesis of Quinazolin-4(3H)-ones with N-Methoxyamides as Synthesis Reagents>, Related Products of 162046-61-9, the main research area is methoxy aryl quinazolinone preparation.

A practical method to synthesize quinoxalinones I [R = H, 6-Me, 7-Et, etc.; R1 = H, 3-Br, 3-MeO, etc.] via intra/intermol. amination using rhodium as the catalyst was developed. A wide variety of quinoxalinones I were prepared from N-methoxybenzamides in moderate to excellent yields. Gram-scale reactions were also achieved, highlighting the synthetic importance of this new transformation.

Synthesis published new progress about Amination. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Related Products of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Chen, Sheng-Ren; Ke, Yi-Yu; Yeh, Teng-Kuang; Lin, Shu-Yu; Ou, Li-Chin; Chen, Shu-Chun; Chang, Wan-Ting; Chang, Hsiao-Fu; Wu, Zih-Huei; Hsieh, Chih-Chien; Law, Ping-Yee; Loh, Horace H.; Shih, Chuan; Lai, Yiu-Kay; Yeh, Shiu-Hwa; Ueng, Shau-Hua published the artcile< Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists>, SDS of cas: 162046-61-9, the main research area is analgesic pain tetrahydroisoquinolinylmethylbenzamide opioid receptor agonist pharmacokinetics; Anti-nociceptive effects; Blood-brain barrier; Penetration; Structure-activity relationship; Tail-flick test; κ-opioid receptor agonist; μ-opioid receptor agonist.

μ-Opioid receptor (MOR) agonists are analgesics used clin. for the treatment of moderate to severe pain, but their use is associated with severe adverse effects such as respiratory depression, constipation, tolerance, dependence, and rewarding effects. In this study, the authors identified I as a novel opioid receptor agonist by high-throughput screening. Structural modifications made to I to improve potency and blood-brain-barrier (BBB) penetration resulted in compounds II and III. Compound II was a potent MOR/KOR (κ-opioid receptor) agonist, and compound III was a potent MOR and medium KOR agonist. Both II and III demonstrated a significant antinociceptive effect in a tail-flick test performed in wild type (WT) B6 mice. The ED50 value of III was 1.059 mg/kg, and the brain concentrations of II and III were 7424 and 11696 ng/g, resp. Accordingly, compounds II and III are proposed for lead optimization and in vivo disease-related pain studies.

European Journal of Medicinal Chemistry published new progress about Analgesics. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, SDS of cas: 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lukesh, John C.; Carney, Daniel W.; Dong, Huijun; Cross, R. Matthew; Shukla, Vyom; Duncan, Katharine K.; Yang, Shouliang; Brody, Daniel M.; Brutsch, Manuela M.; Radakovic, Aleksandar; Boger, Dale L. published the artcile< Vinblastine 20' Amides: Synthetic Analogues That Maintain or Improve Potency and Simultaneously Overcome Pgp-Derived Efflux and Resistance>, Application In Synthesis of 162046-61-9, the main research area is vinblastine amide preparation antitumor.

A series of 180 vinblastine 20′ amides were prepared in three steps from com. available starting materials, systematically exploring a typically inaccessible site in the mol. enlisting a powerful functionalization strategy. Clear structure-activity relationships and a structural model were developed in the studies which provided many such 20′ amides that exhibit substantial and some even remarkable enhancements in potency, many that exhibit further improvements in activity against a Pgp overexpressing resistant cancer cell line, and an important subset of the vinblastine analogs that display little or no differential in activity against a matched pair of vinblastine sensitive and resistant (Pgp overexpressing) cell lines. The improvements in potency directly correlated with target tubulin binding affinity, and the reduction in differential functional activity against the sensitive and Pgp overexpressing resistant cell lines was found to correlate directly with an impact on Pgp-derived efflux.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Application In Synthesis of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Akama, Tsutomu; Dong, Chen; Virtucio, Charlotte; Freund, Yvonne R.; Chen, Daitao; Orr, Matthew D.; Jacobs, Robert T.; Zhang, Yong-Kang; Hernandez, Vincent; Liu, Yang; Wu, Anne; Bu, Wei; Liu, Liang; Jarnagin, Kurt; Plattner, Jacob J. published the artcile< Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents>, Application In Synthesis of 162046-61-9, the main research area is benzoxaborole amid preparation structure activity relationship antiinflammatant; Anti-inflammatory; Benzoxaborole; Collagen-induced arthritis; Cytokine; Interleukin-1beta; Interleukin-6; Pharmacokinetics; Structure–activity relationships; Tumor necrosis factor-alpha.

Structure-activity relationships of 6-(benzoylamino)benzoxaborole analogs were investigated for the inhibition of TNF-α, IL-1β, and IL-6 from lipopolysaccharide stimulated peripheral blood mononuclear cells. One compound showed potent activity against all three cytokines with IC50 values between 0.19-0.50 μM, inhibited LPS-induced TNF-α and IL-6 elevation in mice and improved collagen-induced arthritis in mice. This compound is considered to be a promising lead for novel anti-inflammatory agent with an excellent pharmacokinetic profile.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Application In Synthesis of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zeng, Jie; Zhang, Zhijun; Zhu, Qi; Jiang, Zhiyan; Zhong, Guohua published the artcile< Simplification of natural β-carboline alkaloids to obtain indole derivatives as potent fungicides against rice sheath blight>, Safety of 2-(Trifluoromethoxy)benzoyl chloride, the main research area is indole preparation Agrochem fungicide SAR; Rhizoctonia solani; fungicidal activity; indole; simplification; β-carboline.

The increasing resistance of rice sheath blight caused by Rhizoctonia solani highlights the need for highly effective and environmentally benign agents. Natural β-carboline alkaloids were simplified to obtain a series of indole derivatives, and their fungicidal activity and preliminary mode of action against R. solani were also evaluated. The initial hit indole displayed significant fungicidal activity with an EC50 value of 25.56μg/mL, and was selected for further optimization. Importantly, compound 4-fluroindole the most active compound, had an EC50 value of 0.62μg/mL, and approx. 300-fold more potent than validamycin A (EC50 = 183.00μg/mL). In-vivo bioassay also demonstrated that compound 4-fluoroindole showed better fungicidal activities than validamycin A. Moreover, the mechanism studies revealed that compound 4-fluoroindole not only caused remarkable morphol. and structural alterations of R. solani hyphae, but also induced the loss of mitochondrial membrane potential and interfered with DNA synthesis. Therefore, compound 4-fluoroindole showed superior fungicidal activity against R. solani, and the elucidated mode of action supported the potential application of compound 4-fluoroindole against rice sheath blight.

Molecules published new progress about Agrochemical fungicides. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Safety of 2-(Trifluoromethoxy)benzoyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tu, Guangliang; Wang, Dongjie; Yuan, Chunchen; Zhang, Jingyu; Zhao, Yingsheng published the artcile< Palladium-Catalyzed Para-Selective Difluoromethylation of Arene Esters>, Related Products of 162046-61-9, the main research area is palladium catalyzed regioselective fluoromethylation arene ester.

Highly efficient, palladium-catalyzed, para-selective difluoromethylation of arene esters has been developed using [1,1′-biphenyl-2-yl]dicyclohexylphosphine as the effective ligand. A wide variety of arene esters bearing various functional groups were all compatible with the reaction conditions, leading to para-difluoromethylated products in moderate to good yields. Moreover, benzamide and benzenesulfonamide were also well-tolerated, suggesting that this novel catalyst system has broad applications to a variety of substrates.

Journal of Organic Chemistry published new progress about Arenesulfonamides Role: RCT (Reactant), RACT (Reactant or Reagent). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Related Products of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gillespie, Roger J.; Bamford, Samantha J.; Gaur, Suneel; Jordan, Allan M.; Lerpiniere, Joanne; Mansell, Howard L.; Stratton, Gemma C. published the artcile< Antagonists of the human A2A receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides>, Formula: C8H4ClF3O2, the main research area is pyrimidine carboxamide preparation Parkinson disease antiparkinsonian; pyrimidinylamine arylcarboxylic chloride pyrimininylcarboxylic acid amine amidation; human A1 A2A A2B A3 receptor antagonist structure activity.

A novel series of antagonists of the human A2A receptor have been identified and have been shown to display good potency and high degrees of selectivity over other receptor sub-types. Displaying in vivo potency in commonly used disease models and high oral bio-availability, this class of compounds may serve as clin. useful treatments for the relief of the symptoms associated with Parkinson’s disease.

Bioorganic & Medicinal Chemistry Letters published new progress about Adenosine A1 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Formula: C8H4ClF3O2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Al-Masum, Mohammad; Legan, Sarah; Liu, Kwei-Yu published the artcile< Pd-catalyzed microwave irradiated regioselective aroylation reaction of crotyl- and allyltrifluoroborates>, Quality Control of 162046-61-9, the main research area is alkenone preparation regioselective diastereoselective chemoselective microwave irradiation; trifluoroborate salt aroyl chloride aroylation palladium catalyst.

An interesting regioselectivity is observed when the mixture of potassium crotyltrifluoroborate and aroyl chlorides RC(O)Cl (R = 3,4,6-trifluorophenyl, naphth-2-yl, 4-bromophenyl, etc.) having electron-deficient and electron-rich groups is microwaved in the presence of palladium-catalyst. In the case of electron withdrawing group with Ph ring of aroyl chlorides, isomerized α,β-unsaturated compound RC(O)CH(CH3)=CHCH3 is a product, whereas the electron donating group with Ph ring of aroyl chlorides furnishes α-adduct RC(O)CH(CH3)CH=CH2. Similar aroylation reaction is also established for potassium allyltrifluoroborate. In this case, regioselectivity is unaffected with changing electron-rich or electron-deficient groups in Ph ring of the aroyl chlorides. Reactions proceed with, essentially in same rate, to afford the corresponding aryl propenyl ketones (crotonophenones) RC(O)CH=CHCH3 in good to high yields.

International Journal of Organic Chemistry published new progress about Aromatic acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Quality Control of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Flaherty, Daniel P.; Simpson, Denise S.; Miller, Melissa; Maki, Brooks E.; Zou, Beiyan; Shi, Jie; Wu, Meng; McManus, Owen B.; Aube, Jeffrey; Li, Min; Golden, Jennifer E. published the artcile< Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold>, Recommanded Product: 2-(Trifluoromethoxy)benzoyl chloride, the main research area is bis amide derivative preparation TASK1 potassium channel inhibitor; Bis-amide; KCNK3; Selective potassium channel inhibitor; TASK1.

TASK-1 is a two-pore domain potassium channel that is important to modulating cell excitability, most notably in the context of neuronal pathways. In order to leverage TASK-1 for therapeutic benefit, its physiol. role needs better characterization; however, designing selective inhibitors that avoid the closely related TASK-3 channel has been challenging. In this study, a series of bis-amide derived compounds were found to demonstrate improved TASK-1 selectivity over TASK-3 compared to reported inhibitors. Optimization of a marginally selective hit led to analog 35 which displays a TASK-1 IC50 = 16 nM with 62-fold selectivity over TASK-3 in an orthogonal electrophysiol. assay.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Recommanded Product: 2-(Trifluoromethoxy)benzoyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Thur, Yithachu; Bhalerao, Amit; Munshi, Zaki; Pansare, Nisha; Mann, Klaus; Hanauer, Guido; Kley, Hans-Peter; Nappe, Sandra; Weiss-Haljiti, Cornelia; Ostermann, Claude; Zitt, Christof; Schaefer, Michaela; Mondal, Dibyendu; Ali Siddiki, Afsar; Armugam, Velavan; Gudaghe, Vinod; Gupta, Mahendra; Rayudu, Pramila; Dautzenberg, Frank M.; Das Sarma, Koushik published the artcile< Structure-activity relationships of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists and their analgesic action>, Category: chlorides-buliding-blocks, the main research area is thienopyrancarboxamide preparation cannabinoid receptor analgesic SAR.

SAR studies were performed on a series of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists. Starting from a HTS hit both potency and selectivity could be improved. Modifications to the thiophene fusion and C-3 amides were studied. A representative compound 3t (I) produced analgesia when dosed orally in inflammatory pain models of writhing and carrageenan-induced allodynia.

Bioorganic & Medicinal Chemistry Letters published new progress about Allodynia. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics