- Synthesis of 2,3-disubstituted indoles by a rhodium-catalyzed aromatic amino-claisen rearrangement of N-propargyl anilines
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(Chemical Equation Presented) Give me a ring! A cationic RhI catalyst promotes the formation of fused arenes containing a five-membered ring (see scheme) by an aromatic amino-Claisen rearrangement of N-propargyl aniline derivatives in refluxing
- Saito, Akio,Kanno, Ayumi,Hanzawa, Yuji
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- N-Alkylation of Amines with Alcohols Catalyzed by Manganese(II) Chloride or Bromopentacarbonylmanganese(I)
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A manganese-catalyzed N-alkylation reaction of amines with alcohols via hydrogen autotransfer strategy has been demonstrated. The developed practical catalytic system including an inexpensive, nontoxic, commercially available MnCl2 or MnBr(CO)5 as the metal salt and triphenylphosphine as a ligand provides access to diverse aromatic, heteroaromatic, and aliphatic secondary amines in moderate-to-high yields. In addition, this operationally simple protocol is scalable to the gram level and suitable for synthesizing heterocycles such as indole and resveratrol-derived amines known to be active for Alzheimer's disease.
- Wei, Dongyue,Yang, Peng,Yu, Chuanman,Zhao, Fengkai,Wang, Yilei,Peng, Zhihua
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p. 2254 - 2263
(2021/02/26)
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- Preparation method of polyfluoroaniline
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The invention relates to a preparation method of polyfluoroaniline, according to the method, the polyfluoroaniline is prepared by a two-step common reaction from polyfluorobenzene as a raw material, the method has the characteristics of low reaction temperature, small pressure, low cost, and the like, is suitable for industrial production application, and is convenient for large-scale production;the polyfluoroaniline product obtained by the method has less impurities and high product purity.
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Paragraph 0038-0045
(2018/08/03)
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- Mechanism and Scope of Base-Controlled Catalyst-Free N-Arylation of Amines with Unactivated Fluorobenzenes
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A general method for transition metal-free N-arylation of amines has been developed. Mechanistic studies have revealed that the ability of the base to facilitate the desired amination without promoting unwanted side reactions is the guiding factor. By employing lithium bis(trimethylsilyl)amide as a base the resultant deprotonated amines readily react with a range of unactivated fluorobenzene derivatives. This new arylation method is utilized for the simple two-step synthesis of the antidepressant Vortioxetine.
- Borch Jacobsen, Christian,Meldal, Morten,Diness, Frederik
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supporting information
p. 846 - 851
(2017/02/05)
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- ARYLATION OF ALIPHATIC AMINES
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The invention relates to a method for arylation of amines, such as aliphatic amines by reaction of aryl-halogens, e.g. chloro- or fluorobenzene derivatives without strongly electron withdrawing substituents in the presence of a strong base.
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Page/Page column 27; 32; 33
(2017/09/07)
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- Rhodium(I)-catalyzed synthesis of indoles: Amino-claisen rearrangement of N-propargylanilines
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Mild and facile preparations of 2-substituted or 2,3-disubstituted indole compounds were achieved by RhH(CO)(Ph3P)3 (4-10 mol %)-catalyzed reaction of N-propargylanilines in hexafluoroisopropyl alcohol (HFIP). The formation of indole
- Saito, Akio,Oda, Shoko,Fukaya, Haruhiko,Hanzawa, Yuji
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supporting information; experimental part
p. 1517 - 1524
(2009/07/17)
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- Method of topically treating inflammation
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This invention describes a method of treating inflammation in warmblooded animals by topically administering an effective amount of benzylamine and its derivatives.
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