- A method for preparing 2, 4, 5 - trichloro phenol (by machine translation)
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The invention discloses a 2, 4, 5 - trichloro phenol industrial preparation method. The 2, 4, 5 - trichloro phenol industrial preparation method, in order to 2, 4 - dichloro nitrobenzene is used as the initial raw materials, by chlorine, reduction and diazo - sandmaier three-step reaction synthesis of 2, 4, 5 - trichloro phenol. The got in the course of 2, 4, 5 - trichloro phenol as yellow solid, purity 97.5%, each step the raw material conversion rate respectively reaches 100%, the whole process of the total yield up to 60%. (by machine translation)
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Paragraph 0009; 0012
(2019/02/27)
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- METHODS USING HDAC11 INHIBITORS
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The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.
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Paragraph 0553-0554
(2018/05/16)
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- A novel bis(pinacolato)diboron-mediated N-O bond deoxygenative route to C6 benzotriazolyl purine nucleoside derivatives
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Reaction of amide bonds in t-butyldimethylsilyl-protected inosine, 2′-deoxyinosine, guanosine, 2′-deoxyguanosine, and 2-phenylinosine with commercially available peptide-coupling agents (benzotriazol-1H-yloxy)tris(dimethylaminophosphonium) hexafluorophosphate (BOP), (6-chloro-benzotriazol-1H-yloxy)trispyrrolidinophosphonium hexafluorophosphate (PyClocK), and (7-azabenzotriazol-1H-yloxy)trispyrrolidinophosphonium hexafluorophospate (PyAOP) gave the corresponding O6-(benzotriazol-1-yl) nucleoside analogues containing a C-O-N bond. Upon exposure to bis(pinacolato)diboron and base, the O6-(benzotriazol-1-yl) and O6-(6-chlorobenzotriazol-1-yl) purine nucleoside derivatives obtained from BOP and PyClocK, respectively, underwent N-O bond reduction and C-N bond formation, leading to the corresponding C6 benzotriazolyl purine nucleoside analogues. In contrast, the 7-azabenzotriazolyloxy purine nucleoside derivatives did not undergo efficient deoxygenation, but gave unsymmetrical nucleoside dimers instead. This is consistent with a prior report on the slow reduction of 1-hydroxy-1H-4-aza and 1-hydroxy-1H-7-azabenzotriazoles. Because of the limited number of commercial benzotriazole-based peptide coupling agents, and to show the applicability of the method when such coupling agents are unavailable, 1-hydroxy-1H-5,6-dichlorobenzotriazole was synthesized. Using this compound, silyl-protected inosine and 2′-deoxyinosine were converted to the O6-(5,6-dichlorobenzotriazol-1-yl) derivatives via in situ amide activation with PyBroP. The O6-(5,6-dichlorobenzotriazol-1-yl) purine nucleosides so obtained also underwent smooth reduction to afford the corresponding C6 5,6-dichlorobenzotriazolyl purine nucleoside derivatives. A total of 13 examples were studied with successful reactions occurring in 11 cases (the azabenzotriazole derivatives, mentioned above, being the only unreactive entities). To understand whether these reactions are intra or intermolecular processes, a crossover experiment was conducted. The results of this experiment as well as those from reactions conducted in the absence of bis(pinacolato)diboron and in the presence of water indicate that detachment of the benzotriazoloxy group from the nucleoside likely occurs, followed by reduction, and reattachment of the ensuing benzotriazole, leading to products.
- Basava, Vikram,Yang, Lijia,Pradhan, Padmanava,Lakshman, Mahesh K.
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p. 7069 - 7083
(2016/07/30)
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- Click chemistry inspired facile synthesis and bioevaluation of novel triazolyl analogs of Ludartin
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A convenient and modular synthesis involving diastereoselective Michael addition followed by regioselective Huisgen 1,3-dipolar cycloaddition reaction was carried out to furnish 1,4-disubstituted-1,2,3-triazoles of Ludartin. This reaction scheme involving Michael addition followed by regioselective Huisgen 1,3-dipolar cycloaddition reaction leading to the formation of triazolyl analogs is being reported for the first time. All the triazolyl products were characterised using spectral data analysis. Sulphorhodamine B cytotoxicity screening of the resulting products against a panel of five human cancerous cell-lines revealed that few of the analogs display promising broad spectrum cytotoxic effect. Among all the synthesized compounds, only 3q displayed the best cytotoxic effect with IC50 values of 12, 11, 38, 39 and 8.5 μM but less than the standard Ludartin (1) with IC50 values of 6.3, 7.4, 7.5, 6.9 and 0.5 μM against human neuroblastoma (T98G), lung (A-549), prostate (PC-3), colon (HCT-116) and breast (MCF-7) cancer cell lines, respectively. The present synthesis was designed based on the previous literature reports of Ludartin as an aromatase inhibitor. Our work provides an initial study on structure-activity relationship of triazolyl analogs of sesquiterpene lactones in general and Ludartin (1) in particular.
- Lone, Shabir H.,Bhat, Khursheed A.,Majeed, Rabiya,Hamid, Abid,Khuroo, Mohd A.
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p. 1047 - 1051
(2014/03/21)
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- Model Systems for Flavoenzyme Activity: Relationships between Cofactor Structure, Binding and Redox Properties
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A series of flavins were synthesized bearing electron-withdrawing and -donating substituents. The electrochemical properties of these flavins in a nonpolar solvent were determined. The recognition of these flavins by a diamidopyridine (DAP) receptor and the effect this receptor has on flavin redox potential was also quantified. It was found that the DAP-flavin binding affinity and the reduction potentials (E1/2) for both the DAP-bound and unbound flavins correlated well with functions derived from linear free energy relationships (LFERs). These results provide insight and predictive capability for the interplay of electronics and redox state-specific interactions for both abiotic and enzymatic systems.
- Legrand, Yves-Marie,Gray, Mark,Cooke, Graeme,Rotello, Vincent M.
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p. 15789 - 15795
(2007/10/03)
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- 2-amino-5,6-dichlorobenzimidazole derivatives having antiviral activity
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The present invention relates to benzimidazole derivatives of formula (I) wherein: R1 represents H, C1-4 alkyl, C3-5 cycloalkyl; R2 represents H, C1-4 alkyl; or R1 and R2 together form with the nitrogen a 4 or 5 membered heterocyclic ring; R3 represents BR4 or R4 wherein B represents a bridging group --C(O)NH--, --C(O)NC1-4 alkyl-, or C(O)O-- and R4 represents H, C1-4 alkyl, C2-6 alkenyl or halo (preferably fluoro); and each n is an integer independently selected from 0, 1, or 2 (preferably 0 or 1); and geometric isomers or mixtures thereof; and physiologically functional derivatives thereof, and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to their preparation and pharmaceutical formulations containing them.
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- Ozone-mediated reaction of polychlorobenzenes and some related halogeno compounds with nitrogen dioxide: A novel non-acid methodology for the selective mononitration of moderately deactivated aromatic systems
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In the presence of ozone and preferably methanesulfonic acid as catalyst, polychlorobenzenes undergo selective mononitration with nitrogen dioxide at low temperatures, giving the corresponding polychloronitrobenzenes, in most cases in nearly quantitative yields.
- Suzuki,Mori,Maeda
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p. 841 - 845
(2007/10/02)
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- Preparation of 2,4,5-trichlorophenol and 2,4,5-trichlorophenoxyacetic acid free of 2,3,7,8-tetrachloro-dibenzo-p-dioxin contamination
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A process for the preparation of 2,4,5-trichlorophenol and 2,4,5-trichlorophenoxyacetic acid free of 2,3,7,8-tetrachloro-dibenzo-p-dioxin contamination by the steps of nitrating 1,2,4-trichlorobenzene, reducing the resulting 1,2,4-trichloro-5-nitrobenzene, diazotizing the resulting 2,4,5-trichloroaniline, hydrolyzing the resulting 2,4,5-trichlorobenzenediazonium salt and recovering 2,4,5-trichlorophenol. The 2,4,5-trichlorophenol is reacted with monochloroacetic acid to give 2,4,5-trichlorophenoxyacetic acid. Both the 2,4,5-trichlorophenol and the 2,4,5-trichlorophenoxyacetic acid produced by the process are analytically free of 2,3,7,8-tetrachloro-dibenzo-p-dioxin in analytical tests sensitive to 1 part per billion.
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- Solid-liquid phase transfer catalysis improved method of preparing 2,4-difluoroaniline
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A method of preparing 2,4-difluoroaniline by reacting 2,4,5-trichloronitrobenzene with a fluorinating agent in the presence of a solid-liquid phase interface, and utilizing a phase transfer catalyst to form 2,4-difluoro-5-chloronitrobenzene, followed by hydrogenation with hydrogen in the presence of a hydrogenation catalyst to form 2,4-difluoroaniline.
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