- Coordinating Activation Strategy-Induced Selective C?H Trifluoromethylation of Anilines
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A simple protocol for the synthesis of 2-(trifluoromethyl)aniline derivatives through a coordinating activation strategy was developed. The reaction showed good reactivity and gave the target products in moderate to good yields. Pleasingly, the directing group could be recovered in excellent yield. Furthermore, this strategy allowed efficient access to the synthesis of floctafenine. A single-electron-transfer mechanism was proposed to be responsible for this trifluoromethylation reaction.
- Xu, Jun,Cheng, Ke,Shen, Chao,Bai, Renren,Xie, Yuanyuan,Zhang, Pengfei
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- QUINOXALINE DERIVATIVES
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The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
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- Deoxofluorination of (Hetero)aromatic Acids
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Diverse trifluoromethyl-substituted compounds were synthesized by deoxofluorination of cinnamic and (hetero)aromatic carboxylic acids with sulfur tetrafluoride. The obtained products were used as starting materials in the preparation of novel fluorinated amino acids, anilines, and aliphatic amines - valuable building blocks for medicinal chemistry and agrochemistry.
- Alekseenko, Anatoliy N.,Bugera, Maksym Ya.,Gerus, Igor I.,Kiriakov, Oleksandr,Klipkov, Anton A.,Mykhailiuk, Pavel K.,Pustovit, Yurii,Razhyk, Bohdan,Semenov, Sergey,Starova, Viktoriia S.,Tananaiko, Oksana Yu.,Tarasenko, Karen,Tolmachev, Andrei A.,Trofymchuk, Serhii,Zaporozhets, Olga A.
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p. 3110 - 3124
(2020/03/23)
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- ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
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Paragraph 0133; 0134; 0135
(2017/04/18)
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- Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors
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Abstract A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure-activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK inhibitors. Among them, 29a showed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model. Graphical abstract
- Zhang, Peilong,Dong, Jiaqiang,Zhong, Boyu,Zhang, Deyi,Jin, Can,Meng, Xuejing,Sun, Desheng,Xu, Xiangyuan,Zhou, Yong,Liang, Zhi,Ji, Minghua,Li, Hailong,Xu, Tao,Song, Guowei,Zhang, Ling,Chen, Gang,Yuan, Hongbin,Shih, Joe,Zhang, Ruihao,Hou, Guojun,Jin, Ying,Yang, Qiong
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p. 3738 - 3743
(2015/08/06)
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- Reactions of Trifluoromethyl Bromide and Related Halides: Part 10. Perfluoroalkylation of Aromatic Compounds induced by Sulphur Dioxide Radical Anion Precursors
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Perfluoroalkylation of electron-rich aromatic compounds with trifluoromethyl bromide, or long-chain perfluoroalkyl iodides, was performed in the presence of sodium dithionite or zinc-sulphur dioxide.This alkylation occurred at the ortho and para positions relative to the amino or hydroxy substitutent.Pyrroles were perfluoroalkylated regioselectively at the 2-position.This alkylation was interpreted as a radical aromatic substitution; the formation of the perfluoroalkyl radical can be induced by a single-electron transfer from sulphur dioxide radical anion to the perfluoroalkyl halide.
- Tordeux, Marc,Langlois, Bernard,Wakselman, Claude
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p. 2293 - 2299
(2007/10/02)
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- Process for perfluoroalkylation of aromatic derivatives
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A process for the perfluoroalkylation of aromatic derivatives. In a first stage, an aromatic derivative, sulfur dioxide and a metal selected from the group consisting of zinc, aluminum, manganese, cadmium, magnesium, tin, iron, nickel and cobalt, are brought into contact in a solvent, preferably a polar aprotic solvent. In a second stage, a perfluoroalkyl bromide or iodide is added to react with the aromatic derivative.
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