- Palladium-catalyzed direct and regioselective C-H bond functionalization/ oxidative acetoxylation of indoles
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The first general examples of palladium-catalyzed direct and selective oxidative C3-acetoxylation of indoles are presented. The mild reaction conditions (70 °C and with weak base, KOAc) in this indole C-H-acetoxylation are notable.
- Choy, Pui Ying,Lau, Chak Po,Kwong, Fuk Yee
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supporting information; experimental part
p. 80 - 84
(2011/03/22)
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- Mild copper-catalyzed N-arylation of azaheterocycles with aryl halides
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A highly efficient copper(I)-catalyzed N-arylation of azaheterocycles with various aryl halides is reported. The N-arylation reaction can be carried out using as low as 0.5 mol % of (Cu(I)OTf)2?PhH and 1.0 mol % of 4,7-dichloro-1,10-phenanthrol
- Kuil, Mark,Bekedam, E. Koen,Visser, Gerben M.,Van Den Hoogenband, Adri,Terpstra, Jan Willem,Kamer, Paul C.J.,Van Leeuwen, Piet W.N.M.,Van Strijdonck, Gino P.F.
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p. 2405 - 2409
(2007/10/03)
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- Design and synthesis of subtype-selective cyclooxygenase (COX) inhibitors derived from thalidomide
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A series of substituted indoline and indole derivatives with cyclooxygenase (COX)-inhibitory activity was prepared during our structural development studies based on thalidomide as a multi-template lead compound. Structure-activity relationship studies in
- Sano, Hiroko,Noguchi, Tomomi,Tanatani, Aya,Hashimoto, Yuichi,Miyachi, Hiroyuki
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p. 3079 - 3091
(2007/10/03)
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- Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds
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The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.
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