- Pd-Catalyzed Intramolecular Chemoselective C(sp2)-H and C(sp3)-H Activation of N-Alkyl- N-arylanthranilic Acids
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A controllable palladium-catalyzed intramolecular C-H activation of N-alkyl-N-arylanthranilic acids has been developed. The methodology allows selective synthesis of 1,2-dihydro-(4H)-3,1-benzoxazin-4-ones and carbazoles from the same starting materials and palladium catalyst. The selectivity is controlled by the oxidant. Silver oxide promotes C(sp3)-H activation/C-O cyclization to provide 1,2-dihydro-(4H)-3,1-benzoxazin-4-ones, while copper acetate contributes to C(sp2)-H activation/decarboxylative arylation to afford carbazoles. This protocol is demonstrated by its wide substrate scope and good functional group tolerance.
- Hu, Zhe-Yao,Zhang, Yan,Li, Xin-Chang,Zi, Jing,Guo, Xun-Xiang
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p. 989 - 992
(2019/05/16)
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- A process for preparing 1, 2 - dihydro - (4 H) - 3, 1 - benzoxazin -4 - ketone compound method
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The invention discloses a method for utilizing N - methyl - N - aryl anthranilic acid compound synthesis of 1, 2 - dihydro - (4 H) - 3, 1 - benzoxazin - 4 - ketone compounds, the synthetic method is: the palladium salt as a catalyst, the N - methyl - N -
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Paragraph 0028-0035
(2019/04/14)
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- Organocatalytic enantioselective amination of 2-substituted indolin-3-ones: A strategy for the synthesis of chiral α-hydrazino esters
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An efficient enantioselective α-amination of 2-substituted 3-indolinones has been achieved for the first time using hydroquinidine as a chiral catalyst through an aza-Michael reaction. The desired α-hydrazino esters are obtained in excellent yields with h
- Yarlagadda, Suresh,Ramesh,Ravikumar Reddy,Srinivas,Sridhar,Subba Reddy
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supporting information
p. 170 - 173
(2017/11/27)
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- Substrate-Controlled Selectivity Switch in the Three-Component Coupling Involving Arynes, Aromatic Tertiary Amines, and CO2
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The transition-metal-free multicomponent coupling involving arynes, aromatic tertiary amines, and CO2 is reported. The reaction exhibits switchable selectivity depending on the electronic nature of the aromatic amines used. With amines bearing electron-releasing/neutral groups as the nucleophilic trigger, the reaction afforded 2-arylamino benzoates via a nitrogen to oxygen alkyl group migration. Employing electron-deficient amines in the reaction furnished 2-aminoaryl benzoates proceeding via the aryl to aryl amino group migration resembling a Smiles rearrangement.
- Bhojgude, Sachin Suresh,Roy, Tony,Gonnade, Rajesh G.,Biju, Akkattu T.
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supporting information
p. 5424 - 5427
(2016/11/04)
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- Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6- fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5-trimethyl-4- thiazolidinone maleate
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HP-236 (3-[4-[4-(6-Fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone maleate; P-9236) (54) displayed a pharmacological profile indicative of potential atypical antipsychotic activity. A series of piperazinyl butyl thiazolidi
- Hrib, Nicholas J.,Jurcak, John G.,Bregna, Deborah E.,Burgher, Kendra L.,Hartman, Harold B.,Kafka, Sharon,Kerman, Lisa L.,Kongsamut, Sam,Roehr, Joachim E.,Szewczak, Mark R.,Woods-Kettelberger, Ann T.,Corbett, Roy
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p. 4044 - 4057
(2007/10/03)
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