- A VERY EFFICIENT PREPARATION OF 1,2-DIKETONES
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Treatment of α-thiomethylketones with CuCl2-CuO in aqueous acetone affords the corresponding 1,2-dicarbonyl compounds.
- Carre, M. C.,Caubere, P.
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- SELECTIVE ANDROGEN RECEPTOR MODULATORS
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This invention provides compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and intermediates useful in the preparation of same.
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Page/Page column 49
(2011/09/14)
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- Photo-irradiation of α-halo carbonyl compounds: A novel synthesis of α-hydroxy- and α,α′-dihydroxyketones
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The reaction of α-halo ketones (α-iodocycloalkanones, α-bromocycloalkanones, α-iodo-β-alkoxy esters, and α-iodoacyclicketones) with irradiation under a high-pressure mercury lamp gave the corresponding α-hydroxyketones in good yields. For α-bromoketones, it was found that α-hydroxylation does not occur. However, α-bromoketones were converted into α-hydroxyketones in the presence of KI. In the case of α,α′-diiodo ketones, α,α′-dihydroxyketones, which up to now have scarcely been reported, were obtained. This reaction affords a new, clean and convenient synthetic method for α-hydroxy- and α,α′- dihydroxyketones.
- Chai, Wen,Takeda, Akihiro,Hara, Makoto,Ji, Shun-Jun,Horiuchi, C. Akira
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p. 2453 - 2463
(2007/10/03)
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- A novel synthesis of α-hydroxy- and α,α′- dihydroxyketone from α-iodo and α,α′-diiodo ketone using photoirradiation
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A novel reaction of α-iodo ketone (α-iodocycloalkanone, α-iodo-β-alkoxy ester, and α-iodoacyclicketone) with irradiation under a high-pressure mercury lamp gave the corresponding α-hydroxyketone in good yields. In the case of α,α′- diiodo ketone, α,α′-dihydroxyketone which little has been reported until now was obtained. This reaction affords a new, clean and convenient synthetic method for α-hydroxy- and α,α′- dihydroxyketone.
- Horiuchi, C. Akira,Takeda, Akinori,Chai, Wen,Ohwada, Kishoh,Ji, Shun-Jun,Takahashi, T. Tomoyoshi
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p. 9307 - 9311
(2007/10/03)
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- Kinetics of edta-catalysed oxidation of some cycloalkanones by pyridinium chlorochromate
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The kinetics of oxidation of some cycloalkanones with pyridinium chlorochromate (PCC) in the presence of ethylenediaminetetraacetic acid (edta) was examined and the rate coefficients evaluated. It seems that the enol form of the cycloalkanone is the active substrate. Studies with acrylonitrile indicate the absence of a free radical pathway. The rate data are consistent with a mechanism in which the cyclic ketone complexes with the Cr(VI)-edta intermediate and the ternary complex decomposes through an intramolecular electron-transfer mechanism in a slow rate-limiting step to yield cyclohexane-1,2-dione as the main product. The addition of edta and its binding to the Cr would presumably change the redox potential of the oxidant resulting in a faster reaction. The order of reactivity, C8 > C6 > C5 > C7 is explained.
- Meenakshisundaram, Subbiah,Markkandan, Ramakrishnan
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p. 1101 - 1119
(2007/10/03)
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- Mechanochemical Oxidation of Organic Model Compounds by Means of Potassium Permanganate
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Systematical investigation of solvent-free oxidations of organic model compounds with potassium permanganate on inorganic carriers leads to conclusion, that mechanochemical stimulation can induce oxidations. In case of the benzyl-type arenes these conversions are selective at good yields. Olefines react to carbonic acids. The presence of water enhances the yield of almost all educts.
- Nuechter, Matthias,Ondruschka, Bernd,Trotzki, Ronald
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p. 720 - 724
(2007/10/03)
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- Conformational and steric effects on the oxidation of some cyclic ketones by pyridinium fluorochromate
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The kinetics of oxidation of cyclohexanone, cyclopentanone, cycloheptanone, cyclooctanone and various alpha substituted cyclohexanones by pyridinium fluorochromate(PFC) has been followed under pseudo-first order conditions in aqueous acetic acid medium in the presence of HClO4. The reaction is first order both in oxidant and substrate. The rate increases linearly with increasing [HClO4]. The salt and solvent influences together indicate the reaction to be an ion-dipole type. The stoichiometry between the substrate and oxidant is 1:2 and the product of oxidation is 1,2-diketone. The relative reactivities of various cyclic ketones have been rationalised on the basis of conformational differences and steric factors.
- Krishna Pillay,Kasthuri
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p. 544 - 548
(2007/10/03)
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- OXIDATION REACTIONS OF CYCLOHEPTANE DERIVATIVES WITH CERIUM (IV) IN PERCHLORIC ACID SOLUTIONS
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The kinetic concentration effect of reagents on the reduction of cerium(IV) by cycloheptene, cycloheptanol and cycloheptanone has been determined.It has been shown that the organic compounds form complexes with cerium(IV).Intermediate and final products of the reactions have been identified.Probable mechanisms of the reactions have been proposed.
- Ignaczak, M.,Deka, M.
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p. 269 - 275
(2007/10/02)
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- Anti-mycoplasma agent
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An anti-mycoplasma agent comprising tropolone, its derivatives, represented by the formula: STR1 (wherein R1 is hydroxy, aliphatic acyloxy, arylacyloxy, arysulfonyloxy, carboxyalkyloxy or its ester, benzoylalkyloxy, alkenyloxy, 1,3-dihydro-3-oxo-1-isobenzofuranyloxy, (2-oxo-5-methyl-1,3-dioxol-4-yl)methyloxy or thiocyanato and R2 is hydrogen, halogen, hydroxy, alkyl or alkoxy) and their salts as an active ingredient, which has potent activity especially against tylosin-resistant mycoplasma both in vitro and in vivo and is effectively used in treating the diseases caused thereby.
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- REGIOSELECTIVE REDUCTIONS OF 2,3-EPOXY ACETALS WITH ZINC-CHLOROTRIMETHYLSILANE AND LITHIUM ALUMINIUM HYDRIDE: CONVENIENT SYNTHESIS OF 1,2 AND 1,3-DIONES
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A variety of 2,3-epoxy acetals have been found to undergo regioselective reductions with zinc-chlorotrimethylsilane and lithium aluminium hydride to give 2-hydroxy and 3-hydroxy acetals respectively.Their oxidation followed by hydrolysis furnished the corresponding 1,2- and 1,3-diones in good yields.
- Vankar, Yashwant D.,Chaudhuri, Narayan C.,Rao, C. Trinadha
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p. 551 - 554
(2007/10/02)
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- Arynic Condensatiopn of Ketone Enolates. 17. New General Access to Benzocyclobutene Derivatives
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Arynic condensation of 1,2-diketone monoketal enolates appeared to be a very simple way to synthesize benzocyclobutene derivatives.X-ray diffraction and 1H NMR spectra allowed us to determine the structure of the new compounds and to propose a mechanism concerning these condensations.Finally, during this work we devised a new and easily performed two-step synthesis of 1,2-diketones.
- Gregoire, Brigitte,Carre, Marie-Christiane,Caubere, Paul
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p. 1419 - 1427
(2007/10/02)
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- POLAROGRAPHIC STUDY ON THE KINETICS AND MECHANISM OF THE HYDROLYSIS OF 1,2-CYCLOHEPTANE DIONE DIOXIME
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In acidic aqueous solutions of 1,2-cycloheptane dione dioxime (heptoxime) the oxime groups are successively hydrolyzed and 1,2-cycloheptane dione monoxime and 1,2-cycloheptane dione are formed.The kinetics of these reactions was studied polarographically both in the absence and presence of an excess of hydroxylamine in perchloric acid of various concentrations (0.05-0.2 M) at 20 deg C.The protonization constant of the heptoxime was also determined from kinetic data.The mechanism of the first hydrolysis step is discussed.
- Manok, F.,Koeszegi, E.,Varhelyi, Cs.
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