54542-07-3Relevant academic research and scientific papers
Rhodium(III)-Catalyzed Oxidative Annulation of Ketoximes with Sulfonamide: A Direct Approach to Indazoles
Wang, Ning,Liu, Lingling,Xu, Wentao,Zhang, Mengye,Huang, Zhibin,Shi, Daqing,Zhao, Yingsheng
supporting information, (2019/01/21)
A rhodium(III)-catalyzed intermolecular C-H amination of ketoxime and iodobenzene diacetate-enabled N-N bond formation in the synthesis of indazoles has been developed. A variety of functional groups were well tolerated, providing the corresponding produc
Rhodium(III)-Catalyzed Oxidative Annulation of Ketoximes with Sulfonamide: A Direct Approach to Indazoles
Wang, Ning,Liu, Lingling,Xu, Wentao,Zhang, Mengye,Huang, Zhibin,Shi, Daqing,Zhao, Yingsheng
supporting information, p. 365 - 368 (2019/01/24)
A rhodium(III)-catalyzed intermolecular C-H amination of ketoxime and iodobenzene diacetate-enabled N-N bond formation in the synthesis of indazoles has been developed. A variety of functional groups were well tolerated, providing the corresponding products in moderate to good yields. Moreover, the nitro-substituted ketoximes are well compatible in this reaction, leading to the corresponding products in moderate to good yields.
Rh(III)-Catalyzed Direct Amination of Aromatic Ketoximes Enabled by Potassium Acetate
Liu, Lingling,Wang, Ning,Dai, Chenyang,Han, Yi,Yang, Shan,Huang, Zhibin,Zhao, Yingsheng
, p. 7857 - 7863 (2019/12/12)
A method to achieve rhodium(III)-catalyzed, potassium acetate enabled intermolecular C–H amination of ketoximes using various benzenesulfonamide, especially 4-nitrobenzenesulfonamide is reported. Various aryl ketoximes substituted with electron-withdrawin
Synthesis of 2-fluorocholine aryl carbonyl compounds
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Paragraph 0095, (2017/02/09)
The invention provides a method for synthesizing 2-fluoroarylcarbonyl compounds, which comprises the following steps: converting arylcarbonyl compounds into corresponding carbonyl oxime ether compounds, mildly implementing aryl hydrocarbon chain direct fluoridation of high-selectivity oximido substituent group ortho-position in the presence of a palladium catalyst, a fluoridation reagent and additives, and finally, rehydrolyzing oxime ethers under the action of acid to obtain the 2-fluoroarylcarbonyl compounds. The fluoridation method has the advantages of mild reaction conditions, high substrate adaptability, high fluoridation selectivity and the like, is simple to operate, and has higher application research value.
NHPI and palladium cocatalyzed aerobic oxidative acylation of arenes through a radical process
Liang, Yu-Feng,Wang, Xiaoyang,Tang, Conghui,Shen, Tao,Liu, Jianzhong,Jiao, Ning
supporting information, p. 1416 - 1419 (2016/01/25)
The NHPI and palladium cocatalyzed radical oxidative acylation of arenes with aldehydes and alcohols as acyl equivalents via selective C-H functionalization has been described. Molecular oxygen, the most environmentally friendly oxidant, was used as the terminal oxidant in this catalytic cycle.
Rhodium-catalyzed directed C-H cyanation of arenes with N-cyano-N-phenyl-p-toluenesulfonamide
Gong, Tian-Jun,Xiao, Bin,Cheng, Wan-Min,Su, Wei,Xu, Jun,Liu, Zhao-Jing,Liu, Lei,Fu, Yao
supporting information, p. 10630 - 10633 (2013/08/23)
A Rh-catalyzed directed C-H cyanation reaction was developed for the first time as a practical method for the synthesis of aromatic nitriles. N-Cyano-N-phenyl-p-toluenesulfonamide, a user-friendly cyanation reagent, was used in the transformation. Many different directing groups can be used in this C-H cyanation process, and the reaction tolerates a variety of synthetically important functional groups.
α-Methylation at benzylic fragment of N-aryl-N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model
Gomtsyan, Arthur,Bayburt, Erol K.,Keddy, Ryan,Turner, Sean C.,Jinkerson, Tammie K.,Didomenico, Stanley,Perner, Richard J.,Koenig, John R.,Drizin, Irene,McDonald, Heath A.,Surowy, Carol S.,Honore, Prisca,Mikusa, Joe,Marsh, Kennan C.,Wetter, Jill M.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 3894 - 3899 (2008/02/09)
SAR studies for N-aryl-N′-benzyl urea class of TRPV1 antagonists have been extended to cover α-benzyl alkylation. Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharmacokinetic properties. Further structural manipulations that included replacement of isoquinoline core with indazole and isolation of single enantiomer led to TRPV1 antagonists like (R)-16a with superior pharmacokinetic properties and greater potency in animal model of inflammatory pain.
