- Photo-nickel dual catalytic benzoylation of aryl bromides
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The dual catalytic arylation of aromatic aldehydes by aryl bromides using UV-irradiation and a nickel catalyst is reported. The reaction product serves as a photocatalyst and a hydrogen atom transfer agent for this transformation.
- Schirmer, Tobias Emanuel,Wimmer, Alexander,Weinzierl, Florian Wolfgang Clemens,K?nig, Burkhard
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supporting information
p. 10796 - 10799
(2019/09/13)
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- Transition-Metal-Free Carbonylative Suzuki-Miyaura Reactions of Aryl Iodides with Arylboronic Acids Using N-Formylsaccharin as CO Surrogate
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Unprecedented, high yielding, transition-metal-free carbonylative Suzuki-Miyaura reactions of aryl iodides with arylboronic acids using N-formylsaccharin as CO surrogate have been developed. Notably, this general protocol was adapted to the synthesis of the triglyceride and cholesterol regulator drug, fenofibrate, and carbon-13 labeled biaryl ketone. (Figure presented.).
- Yu, Dezhong,Xu, Fangning,Li, Dan,Han, Wei
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supporting information
p. 3102 - 3107
(2019/05/21)
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- INDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
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The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.
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Page/Page column 98; 100; 101
(2017/03/14)
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- The transition-metal-catalyst-free oxidative homocoupling of organomanganese reagents prepared by the insertion of magnesium into organic halides in the presence of MnCl2·2LiCl
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Organomanganese reagents were prepared by the insertion of magnesium into aryl halides in the presence of MnCl2·2LiCl. These organomanganese reagents smoothly undergo 1,2-addition, acylation, and Pd-catalyzed cross-coupling with various electrophiles. Especially, the oxidative homocoupling of organomanganese reagents was completed in one pot without an additional transition-metal catalyst.
- Peng, Zhihua,Li, Na,Sun, Xinyang,Wang, Fang,Xu, Lanjian,Jiang, Cuiyu,Song, Linhua,Yan, Zi-Feng
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p. 7800 - 7809
(2014/12/10)
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- Synthesis and structure-activity relationships of benzophenone hydrazone derivatives with insecticidal activity
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A broad range of benzophenone hydrazone derivatives was prepared and tested against selected chewing insect pests, allowing the analysis of structure-activity relationships. Good activity was found only when the aromatic rings were substituted at the 4-positions with an halogen atom and a triflate or perhaloalkoxy group. In contrast, a number of substituents on the hydrazone part led to active compounds, the best results being achieved with acyl-type substituents. The excellent laboratory and greenhouse activity of the best representatives was confirmed in semi-field trials against Spodoptera littoralis. ° 2001 Society of Chemical Industry.
- Boeger, Manfred,Duerr, Dieter,Gsell, Laurenz,Hall, Roger G.,Karrer, Friedrich,Kristiansen, Odd,Maienfisch, Peter,Pascual, Alfons,Rindlisbacher, Alfred
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p. 191 - 202
(2007/10/03)
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- Short synthesis of 4-chloro-4′-(chlorodifluoromethoxy)benzophenone
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A one-pot, highly selective synthesis of 4-chloro-4′-(chlorodifluoromethoxy)benzophenone suitable for an industrial scale-up was developed. Fluorination of 4-(trichloromethoxy)benzoyl chloride at -20°C with HF to 4-(chlorodifluoromethoxy)benzoyl fluoride followed by an in situ Friedel-Crafts reaction with chlorobenzene in the presence of BF3 at -5°C yielded the title compound in excellent yield.
- Karrer, Friedrich,Meier, Hans,Pascual, Alfons
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- Synthesis and insecticidal activity of 4-perhaloalkoxy (or thioalkyl) benzophenonehydrazone derivatives
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Benzophenonehydrazone derivatives containing a mesylate or triflate substituent are known to exhibit insecticidal activity. In the present study, such substituents have been replaced by perhaloalkoxy groups. High levels of activity against lepidopteran pests were observed in greenhouse trials. For optimum activity, the substituents should be relatively small. In semi-field trials, however, none of the compounds tested showed sufficient persistence to warrant further development.
- Duerr, Dieter,Gsell, Laurenz,Hall, Roger G.,Karrer, Friedrich,Pascual, Alfons,Rindlisbacher, Alfred
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p. 584 - 587
(2007/10/03)
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- Acylation du trifluoromethoxybenzene en catalyse HF-BF3
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Friedel and Crafts acylation of trifluoromethoxy- and trifluoromethyl-thiobenzene fails to give ketones in a one step synthesis if chlorinated Lewis acids (AlCl3) are used, because of halogen exchange on the -OCF3 and -SCF3 groups.The use of a fluorinated catalyst system such as HF-BF3 avoids exchange reactions and acylation occurs smoothly under mild conditions: - Low temperature and pressure - High yields (very often >90 percent) - Very high para-regioselectivity.Related reactions such as formylation or sulfonylation can also be achieved under similar conditions.
- Desbois, Michel
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p. 885 - 890
(2007/10/02)
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- Process for the preparation of α,α-difluoroalkyl-thiophenyl ketones
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A process for the preparation of α,α-difluoroalkoxy or α,α-difluoroalkylthiophenyl ketones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a carboxylic acid, a precursor or a derivative of this acid in the presence of boron trifluoride in such an amount that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having phytosanitary (e.g., herbicidal) or pharmaceutical activity.
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