chlorides-buliding-blocks Archives - Page 915 of 1743

Trost, Barry M’s team published research in Angewandte Chemie, International Edition in 2019 | 2382-10-7

Angewandte Chemie, International Edition published new progress about Aldimines Role: RCT (Reactant), RACT (Reactant or Reagent). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, HPLC of Formula: 2382-10-7.

Trost, Barry M.; Jiao, Zhiwei; Hung, Chao-I. published the artcile< Elaborating Complex Heteroaryl-Containing Cycles via Enantioselective Palladium-Catalyzed Cycloadditions>, HPLC of Formula: 2382-10-7, the main research area is methylenecyclopentane methylenepyrrolidine methylenetetrahydrofuran methylenespirotetrahydrofuranindolon stereoselective preparation; palladium diamidophosphite catalyst regioselective stereoselective cycloaddition heteroaryl allylic carbonate; chalcone nitroalkene aldimine aldehyde stereoselective cycloaddition heteroaryl allylic carbonate; asymmetric catalysis; cycloadditions; heterocycles; palladium; trimethylenemethane.

In the presence of allyl(cyclopentadienyl)palladium and a nonracemic diamidophosphite ligand, allylic carbonates containing heteroaryl and nitrophenyl moieties such as I underwent regioselective, diastereoselective, and enantioselective cycloaddition reactions with chalcones, electron-deficient alkenes, aryl aldimines, and nitrobenzaldehydes or N-methylisatin to yield nonracemic methylenecyclopentanes such as II, methylenepyrrolidines, methylenetetrahydrofurans, and methylenespirotetrahydrofuranindolones. Fused and bridged products were also prepared from nitrocycloalkenes and tropone. Allylic carbonates containing many classes of nitrogen-containing aromatics, including pyridines, quinolines, pyrimidines, various azoles and purines, were compatible substrates.

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

Arikawa, Yasuyoshi’s team published research in Journal of Medicinal Chemistry in 2012-05-10 | 5335-40-0

Journal of Medicinal Chemistry published new progress about Digestive tract disease. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Recommanded Product: 3-(Methylsulfonyl)benzenesulfonyl Chloride.

Arikawa, Yasuyoshi; Nishida, Haruyuki; Kurasawa, Osamu; Hasuoka, Atsushi; Hirase, Keizo; Inatomi, Nobuhiro; Hori, Yasunobu; Matsukawa, Jun; Imanishi, Akio; Kondo, Mitsuyo; Tarui, Naoki; Hamada, Teruki; Takagi, Terufumi; Takeuchi, Toshiyuki; Kajino, Masahiro published the artcile< Discovery of a Novel Pyrrole Derivative 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine Fumarate (TAK-438) as a Potassium-Competitive Acid Blocker (P-CAB)>, Recommanded Product: 3-(Methylsulfonyl)benzenesulfonyl Chloride, the main research area is pyrrole fluorophenylpyridinylsulfonyl preparation gastric acid secretion inhibitor; proton potassium ATPase gastric inhibitor pyrrole fluorophenylpyridinylsulfonyl.

In our pursuit of developing a novel and potent potassium-competitive acid blocker (P-CAB), we synthesized pyrrole derivatives focusing on compounds with low log D and high ligand-lipophilicity efficiency (LLE) values. Among the compounds synthesized, the compound I exhibited potent H+,K+-ATPase inhibitory activity and potent gastric acid secretion inhibitory action in vivo. Its maximum efficacy was more potent and its duration of action was much longer than those of proton pump inhibitors (PPIs). Therefore, compound I (1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate, TAK-438) was selected as a drug candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases.

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

Song, Ming-Yu’s team published research in Bioorganic & Medicinal Chemistry in 2017-10-15 | 53581-86-5

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Application In Synthesis of 53581-86-5.

Song, Ming-Yu; Cao, Chen-Yu; He, Qiu-Rui; Dong, Qing-Miao; Li, Ding; Tang, Jiang-Jiang; Gao, Jin-Ming published the artcile< Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions>, Application In Synthesis of 53581-86-5, the main research area is dihydrofuran dihydroisoxazole isocombretastatin analog preparation tubulin polymerization inhibitor; Combretastatin-4; Dihydrofuran; Dihydroisoxazole; Isocombretastatin-4; Tubulin polymerization inhibitors; [3+2] reactions.

[3+2] Reactions play a key role in constructing various pharmaceutical moleculars. In this study, using Mn(OAc)3 mediated and 1,3-dipolar [3+2] cyclization reactions, 38 novel dihydrofuran and dihydroisoxazole analogs of isoCA-4 were synthesized as inhibitors of tubulin polymerization Among them, compound 6g (5-(3-(4-chlorophenyl)-5-(3,4,5-trimethoxyphenyl)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenol) was found to be the most potent cytotoxic agents against PC-3 cells with IC50 value of 0.47 μM, and compound 5p ((5-(3-hydroxy-4-methoxyphenyl)-2-phenyl-5-(3,4,5-trimethoxyphenyl)-4,5-dihydrofuran-3-yl)(phenyl)methanone) exhibted highest activity on HeLa cells with IC50 vaule of 2.32 μM. Tubulin polymerization assay revealed that 6g was a dose-dependent and effective inhibitor of tubulin assembly. Immunohistochem. studies and cell cycle distribution anal. indicated that 6g severely disrupted microtubule network and significantly arrested most cells in the G2/M phase of the cell cycle in PC-3 cells. In addition, mol. docking studies showed that two chiral isomers of 6g can bind efficiently and similarly at colchicine binding site of tubulin.

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

Watanabe, Toshio’s team published research in Journal of Molecular Structure: THEOCHEM in 2004-08-31 | 1435-43-4

Journal of Molecular Structure: THEOCHEM published new progress about Ab initio methods (G2M(RCC)). 1435-43-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H3ClF2, Application In Synthesis of 1435-43-4.

Watanabe, Toshio; Wang, Zun-Yao; Takahashi, Ohgi; Morihashi, Kenji; Kikuchi, Osamu published the artcile< Calculation of systematic set of bond dissociation enthalpies of polyhalogenated benzenes>, Application In Synthesis of 1435-43-4, the main research area is systematic bond dissociation enthalpy polyhalogenated benzene.

The bond dissociation enthalpies (BDEs) of polyhalogenated benzenes were calculated by using the G2M(CC), B3LYP/6-311G(2df,p), and B3LYP/6-311G(d,p) methods. The BDEs of C-H and C-X (X = F, Cl, and Br) calculated by these three methods well reproduced the exptl. BDEs, within 1.2, 2.3, and 4.5 kcal/mol, resp. The anal. of the basis set dependence of the BDEs showed that the BDEs calculated by the B3LYP/6-311G(d,p) method are sufficient for the quant. discussion. An accurate and systematic set of the BDEs of polyhalogenated benzenes was thus obtained by B3LYP/6-311G(d,p) calculations The substitution effects on the BDEs of polyhalogenated benzenes were analyzed by using a linear scheme with and without the correction terms for steric effect. The resulting regression equation for the C-F BDEs well reproduced the calculated C-F BDEs even without the correction term for steric effect, but the regression equations for the C-Cl and C-Br BDEs needs the correction term for steric effect.

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

Liu, Jian’s team published research in Catalysis Science & Technology in 2021 | 3240-10-6

Catalysis Science & Technology published new progress about Adsorption. 3240-10-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H5ClO2, Quality Control of 3240-10-6.

Liu, Jian; Zhang, Xiaoyi; Wen, Bingyan; Li, Yipei; Wu, Jingjing; Wang, Zhipeng; Wu, Ting; Zhao, Rusong; Yang, Shenghong published the artcile< Pre-carbonized nitrogen-rich polytriazines for the controlled growth of silver nanoparticles: catalysts for enhanced CO2 chemical conversion at atmospheric pressure>, Quality Control of 3240-10-6, the main research area is silver polytriazine carboxylation catalyst precarbonization carbon dioxide capture.

High catalytic activity and sufficient durability are two unavoidable key indexes of an efficient heterogeneous catalyst for the direct carboxylation of terminal alkynes with CO2 conversion. Nitrogen-rich covalent triazine frameworks (CTFs) are promising substrates, while random distribution of some residual -NH2 groups brings challenges to the controlled growth of catalytic species. Here, we adopt a pre-carbonization protocol, annealing below the carbonization temperature, to eliminate the random -NH2 groups in CTFs and meanwhile to promote polycondensation degree under the premise of maintaining the pore structure. Benefiting from the improved condensation and orderly N atoms, p-CTF-250, for which CTFs are annealed at 250°C, exhibits improved CO2 adsorption capacity and the ability to control the growth of Ag NPs. Mono-dispersed Ag NPs are generated controllably and entrapped to form Ag@p-CTF-250 catalysts. These Ag@p-CTF-250 catalysts were employed in the direct carboxylation of various terminal alkynes with CO2 under mild conditions (50°C, 1 atm) and showed excellent catalytic activity. In addition, these catalysts have robust recyclability and can be used for at least 5 catalytic runs while retaining yield above 90%. CO2 conversion proceeds well under the synergistic effect between the high CO2 capture capability and the uniform tiny Ag NPs in Ag@p-CTF-250 “”nanoreactors””. The results represent an efficient strategy for controlling the growth of metallic nanoparticles in porous organic polymer substrates containing disordered heteroatoms.

Catalysis Science & Technology published new progress about Adsorption. 3240-10-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H5ClO2, Quality Control of 3240-10-6.

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

Zheng, Bing’s team published research in Advanced Synthesis & Catalysis in 2016 | 1435-43-4

Advanced Synthesis & Catalysis published new progress about Aryl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 1435-43-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H3ClF2, Quality Control of 1435-43-4.

Zheng, Bing; Li, Minyan; Gao, Gui; He, Yuying; Walsh, Patrick J. published the artcile< Palladium-Catalyzed α-Arylation of Methyl Sulfonamides with Aryl Chlorides>, Quality Control of 1435-43-4, the main research area is aryl sulfonamide preparation; methyl sulfonamide aryl chloride palladium catalyst monoarylation; Palladium-catalyzed; aryl chloride; arylation; sulfonamide; sumatriptan.

A palladium-catalyzed α-arylation of sulfonamides with aryl chlorides was presented. A Buchwald-type pre-catalyst formed with Kwong’s indole-based ligand enabled this transformation to be compatible with a large variety of Me sulfonamides and aryl chlorides in good to excellent yields. Importantly, under the optimized reaction conditions, only monoarylated products were observed This method was applied to the efficient synthesis of sumatriptan, which wass used to treat migraines.

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

Dhanya, Raveendra-Panickar’s team published research in Journal of Medicinal Chemistry in 2014-05-22 | 3964-57-6

Journal of Medicinal Chemistry published new progress about Drug dependence. 3964-57-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Reference of 3964-57-6.

Dhanya, Raveendra-Panickar; Sheffler, Douglas J.; Dahl, Russell; Davis, Melinda; Lee, Pooi San; Yang, Li; Nickols, Hilary Highfield; Cho, Hyekyung P.; Smith, Layton H.; D’Souza, Manoranjan S.; Conn, P. Jeffrey; Der-Avakian, Andre; Markou, Athina; Cosford, Nicholas D. P. published the artcile< Design and Synthesis of Systemically Active Metabotropic Glutamate Subtype-2 and -3 (mGlu2/3) Receptor Positive Allosteric Modulators (PAMs): Pharmacological Characterization and Assessment in a Rat Model of Cocaine Dependence>, Reference of 3964-57-6, the main research area is phenoxybutoxy benzoic acid preparation metabotropic glutamate receptor allosteric modulator.

As part of our ongoing small-mol. metabotropic glutamate (mGlu) receptor pos. allosteric modulator (PAM) research, we performed structure-activity relationship (SAR) studies around a series of group II mGlu PAMs. Initial analogs exhibited weak activity as mGlu2 receptor PAMs and no activity at mGlu3. Compound optimization led to the identification of potent mGlu2/3 selective PAMs with no in vitro activity at mGlu1,4-8 or 45 other CNS receptors. In vitro pharmacol. characterization of representative compound I indicated agonist-PAM activity toward mGlu2 and PAM activity at mGlu3. The most potent mGlu2/3 PAMs were characterized in assays predictive of ADME/T and pharmacokinetic (PK) properties, allowing the discovery of systemically active mGlu2/3 PAMs. On the basis of its overall profile, compound II was selected for behavioral studies and was shown to dose-dependently decrease cocaine self-administration in rats after i.p. administration. These mGlu2/3 receptor PAMs have significant potential as small mol. tools for investigating group II mGlu pharmacol.

Journal of Medicinal Chemistry published new progress about Drug dependence. 3964-57-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Reference of 3964-57-6.

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

Yao, Yongqi’s team published research in Organic Chemistry Frontiers in | 672948-03-7

Organic Chemistry Frontiers published new progress about Acyloxylation (regioselective). 672948-03-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H3NO3, Synthetic Route of 672948-03-7.

Yao, Yongqi; Su, Shaoting; Wu, Nan; Wu, Wanqing; Jiang, Huanfeng published the artcile< The cobalt(II)-catalyzed acyloxylation of picolinamides with bifunctional silver carboxylate via C-H bond activation>, Synthetic Route of 672948-03-7, the main research area is picolinamide silver carboxylate cobalt catalyst acyloxylation; acyloxy naphthalenyl picolinamide regioselective preparation.

The cobalt(II)-catalyzed C-H bond acyloxylation of picolinamides with bifunctional silver carboxylate was developed. The operationally simple acyloxylation allowed us to efficiently synthesize 8-functionalized 1-naphthylamine (up to 94% yield) under mild conditions without any addnl. oxidant and base additives. Control experiments were performed to investigate the mechanism of the reaction. This mild and practical acyloxylation approach provide an efficient route for accessing highly functionalized polysubstituted naphthalene compounds and a pathway for modifying drug mols. and natural products.

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

Dana, Srikanta’s team published research in ACS Medicinal Chemistry Letters in 2020-07-09 | 17082-09-6

ACS Medicinal Chemistry Letters published new progress about Antimalarials. 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, Related Products of 17082-09-6.

Dana, Srikanta; Valissery, Praveesh; Kumar, Sharvan; Gurung, Sumiran Kumar; Mondal, Neelima; Dhar, Suman Kumar; Mukhopadhyay, Pritam published the artcile< Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity>, Related Products of 17082-09-6, the main research area is chloroquinolone ciprofloxacin hybrid pharmacophore antimalarial.

Antimalarial drug resistance is a serious obstacle in the persistent quest to eradicate malaria. There is a need for potent chem. agents that are able to act on drug-resistant Plasmodium falciparum populations at reasonable concentrations without any related toxicity to the host. By rational drug design, we envisaged to address this issue by generating a novel hybrid drug possessing two pharmacophores that can act on two unique and independent targets within the cell. We synthesized a new class of ciprofloxacin-based hybrid mols., which have been integrated with acridine, quinolone, sulfonamide, and cinnamoyl pharmacophores. We realized a potent chloroquinolone-ciprofloxacin-based antimalarial hybrid (CQ-CFX) whose mechanism of action is unlike that of its parent mols. indicating a unique biol. target. CQ-CFX is not only potent against CQ-resistant and susceptible strains of Plasmodium falciparum at low nanomolar concentrations (IC50 values are 63.17 ± 1.2 nM and 25.52 ± 4.45 nM, resp.) but is also not toxic to mammalian and bacterial systems up to 20μM and 1μM, resp.

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

Carroll, William A’s team published research in Bioorganic & Medicinal Chemistry Letters in 2007-07-15 | 2905-54-6

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Formula: C8H6Cl2O2.

Carroll, William A.; Kalvin, Douglas M.; Perez Medrano, Arturo; Florjancic, Alan S.; Wang, Ying; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Grayson, George; Honore, Prisca; Jarvis, Michael F. published the artcile< Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists>, Formula: C8H6Cl2O2, the main research area is purinoceptor antagonist analgesic triazole preparation SAR.

Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X7 antagonists were identified with similar potency to the lead compound 4 but with improved physiochem. properties. Compound 12 (I) was active in a rat model of neuropathic pain.

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Formula: C8H6Cl2O2.

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