- Synthesis of Ti-Al binary oxides and their catalytic application for C-H halogenation of phenols, aldehydes and ketones
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Traditional C–H halogenation of organic compounds often requires corrosive agent or harsh condition, and current researches are focused on the use of noble metals as catalyst. In order to give an efficient, benign, activity-adjustable and cost-effective system for halogenation, a series of Ti-Al mixed oxides are prepared as catalyst through sol-gel in this work. Characterizations reveal all catalysts contain more aluminum than titanium, but preparative conditions affect their composition and crystallinity. Monitoring of particle size, zeta potential and UV–vis of preparative solution reveals that formation of catalyst colloids undergoes chemical reaction, affecting catalyst morphology. In halogenation, all catalysts show moderate to high activities, copper chloride proves to be an effective halogen source rather than sodium chloride. The chlorination and bromination are better than iodization, phenol and ketone appear to be more appropriate substrates than aldehyde. Additionally, oxide backbone of catalyst is more durable than its organic components during recycling. This study may provide new catalytic materials for progress of C–H activation.
- Su, Peigen,Fan, Chao,Yu, Heng,Wang, Wanqin,Jia, Xin,Rao, Qifan,Fu, Chenxi,Zhang, Donghua,Huang, Benhua,Pan, Cheng,Zheng, Aqun,Sun, Yang
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- In situ Generation of Hypervalent Iodine Reagents for the Electrophilic Chlorination of Arenes
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Efficient metal-free methods for the electrophilic chlorination of arenes using PIFA and simple chlorine sources are reported. The in situ formation of PhI(Cl)OCOCF3 from PIFA and KCl is proposed, which resulted in a chlorinating species for moderately activated arenes. Moreover, the in situ formation of PhICl2 from PIFA and TMSCl resulted in an excellent approach for the chlorination of a great variety of arenes (20 examples) in high yields, even when working on a multigram scale.
- Granados, Albert,Jia, Zhiyu,del Olmo, Marc,Vallribera, Adelina
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p. 2812 - 2818
(2019/04/08)
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- Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
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The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
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Paragraph 0519
(2015/09/22)
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- 2,4,6-Tris[(4-dichloroiodo)phenoxy)]-1,3,5-triazine as a new recyclable hypervalent iodine(III) reagent for chlorination and oxidation reactions
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The synthesis of 2,4,6-tris[(4-dichloroiodo)phenoxy)]-1,3,5-triazine, as a new recyclable nonpolymeric analogue of (dichloroiodo)benzene, is achieved in two steps using 2,4,6-trichloro-1,3,5-triazine and 4-iodophenol. The application of 2,4,6-tris[(4-dichloroiodo)phenoxy)]-1,3,5-triazine for the chlorination reaction of various activated arenes, olefin, and 1,3-diketone is demonstrated. The reagent 2,4,6-tris[(4-dichloroiodo)phenoxy)]-1,3,5-triazine can be applied also for the oxidative synthesis of 1,3,4-oxadiazoles and 1,2,4-thiadiazoles under mild conditions in excellent yields. The recyclability of the 2,4,6-tris[(4-dichloroiodo)phenoxy)]-1,3,5-triazine was possible owing to the facile recovery and reuse of the coproduced 2,4,6-tris(4-iodophenoxy)-1,3,5- triazine from the reaction mixture due to its practical insolubility in methanol. Georg Thieme Verlag Stuttgart, New York.
- Thorat, Prerana B.,Bhong, Bhagyashree Y.,Karade, Nandkishor Y.
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supporting information
p. 2061 - 2066
(2013/10/21)
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- MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
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- COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES
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The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
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- Synthesis and reactivity of fluorous and nonfluorous aryl and alkyl iodine(III) dichlorides: New chlorinating reagents that are easily recycled using biphasic protocols
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Fluorous aryl and alkyl iodine(III) dichlorides of the formulas (R fn(CH2)3)2C6H 3ICl2 (Rfn ) CF3(CF 2)n-1; n ) 8 for 3,5-disubstituted and n ) 6, 8, 10 for 2,4-disubstituted) and RfnCH2ICl2 (n ) 8, 10) are prepared in 71-98% yields by reactions of Cl2 and the corresponding fluorous iodides. These are effective reagents for the conversions of cyclooctene to trans-1,2-dichlorocyclooctene, anisole to 4-chloro- and 2-chloroanisole, 4-tert-butylphenol to 2-chloro-4-tert-butylphenol, PhCOCH 2COPh to PhCOCHClCOPh, and PhCOCH3 to PhCOCH2Cl and PhCOCHCl2 (CH3CN, rt to 40°C, 100-64% conversions). The chlorinated products and fluorous iodide coproducts are easily separated by organic/fluorous liquid/liquid biphase workups. The latter are obtained in 97-90% yields and reoxidized with Cl2. Analogous chlorinations are conducted with 3-Cl2IC6H4COOH (16) and 4,4'-Cl2IC6H4C6H 4ICl2. With the former, the products and coproduct 3-IC6H4COOH (91-85% recoveries) are easily separated by organic/aqueous NaHCO3 liquid/ liquid biphase workups. The coproduct from the latter, 4,4'-IC6H4C6H4I, is insoluble in common organic solvents, allowing separation by liquid/solid phase workups (91-89% recoveries). The effect of the structure of the iodine(III) dichloride upon reactivity is analyzed in detail. The fluorous systems with Rf8 substituents are generally superior, but 16 is more reactive and gives higher selectivities.
- Podgorsek, Ajda,Jurisch, Markus,Stavber, Stojan,Zupan, Marko,Iskra, Jernej,Gladysz, John A.
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body text
p. 3133 - 3140
(2009/08/15)
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- (2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents
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A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARα agonisim. As a result, highly potent, and selective PPARα agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models.
- Koyama, Hiroo,Boueres, Julia K.,Miller, Daniel J.,Berger, Joel P.,MacNaul, Karen L.,Wang, Pei-Ran,Ippolito, Marc C.,Wright, Samuel D.,Agrawal, Arun K.,Moller, David E.,Sahoo, Soumya P.
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p. 3347 - 3351
(2007/10/03)
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- Novel 2,3-dihydrobenzofuran-2-carboxylic acids: Highly potent and subtype-selective PPARα agonists with potent hypolipidemic activity
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The design and synthesis of a novel class of 2,3-dihydrobenzofuran-2- carboxylic acids as highly potent and subtype-selective PPARα agonists are reported. Systematic study of structure-activity relationships has identified several key structural elements within this class for maintaining the potency and subtype selectivity. Select compounds were evaluated in animal models of dyslipidemia using Syrian hamsters and male Beagle dogs, and all these compounds displayed excellent cholesterol- and triglyceride-lowering activity at dose levels that were much lower than the marketed weak PPARα agonist fenofibrate.
- Shi, Guo Q.,Dropinski, James F.,Zhang, Yong,Santini, Conrad,Sahoo, Soumya P.,Berger, Joel P.,MacNaul, Karen L.,Zhou, Gaochao,Agrawal, Arun,Alvaro, Raul,Cai, Tian-Quan,Hernandez, Melba,Wright, Samuel D.,Moller, David E.,Heck, James V.,Meinke, Peter T.
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p. 5589 - 5599
(2007/10/03)
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- LACTAM COMPOUNDS AND MEDICINAL USE THEREOF
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An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.
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- 2-Hydroxylaminomethyl phenols
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It has been found that certain 4-substituted 2-hydroxylaminomethyl phenols or their nontoxic pharmaceutically acceptable acid addition salts are excellent diuretic, saluretic and anti-inflammatory agents.
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- Sulfuryl Chloride as a Reagent for Selective Chlorination of Symmetrical Ketones and Phenols
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Cyclohexanone reacts with sulfuryl chloride in sulfur dioxide, ether, tetrahydrofuran, dioxane, and tetraglyme to give mixtures of mono- and dichlorocyclohexanones.However, when the reaction was carried out in sulfur dioxide solution containing a slight excess of methanol, only monochlorocyclohexanone was obtained in high yield.Almost as good selectivities are obtained in methylene chloride solution in the presence of methanol.A similar procedure with acetone affords monochloroacetone cleanly.While phenols do not react with sulfuryl chloride in methylene chloride even under reflux, the chlorination can be induced by the addition of various organic "bases", resulting in selective monochlorination.
- Masilamani, Divakar,Rogic, Milorad M.
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p. 4486 - 4489
(2007/10/02)
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