- Synthetic method for 2-methyl-3-trifluoromethylaniline
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The invention discloses a synthetic method for 2-methyl-3-trifluoromethylaniline. The method comprises the following steps: with 2-chloro-3-trifluoromethylaniline as a raw material, introducing a methylthio group onto the 2-chloro-3-trifluoromethylaniline, carrying out a reaction with sulfonyl chloride so as to convert the methylthio group into a chloromethyl group, and carrying out neutralizationand hydrogenation so as to obtain a pure product namely the 2-methyl-3-trifluoromethylaniline. The synthetic method provided by the invention has a synthetic route which is described in the specification. The preparation method provided by the invention adopts more economical raw materials, has simple and convenient preparation process, is free of participation of toxic substances, reaches a yield of 70%, obtains a product with a purity higher than 99%, has good economic significance, and is applicable to large-scale industrial production.
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Paragraph 0028; 0037; 0042-0044; 0049-0050
(2019/01/07)
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- Modular C-H Functionalization Cascade of Aryl Iodides
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We report the first example of ipso-borylation for the modular 1,2-bisfunctionalization of aryl iodides via C-H functionalization. The carbon-boron bond is used as a lynchpin to access ipso carbon-carbon, carbon-nitrogen, carbon-oxygen, and carbon-halogen (Cl, Br, I) bonds. The utility of our methodology is illustrated through quick, modular syntheses of the pharmaceuticals Abilify and Flunixin.
- Shi, Hang,Babinski, David J.,Ritter, Tobias
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supporting information
p. 3775 - 3778
(2015/04/14)
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- Regioselective electrophilic trifluoromethylation of substituted anilines and derivatives in superacid
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In a one pot procedure, treatment of chloro or methyl substituted acetanilides in HF/SbF5/CCl4 followed by addition of HF/pyridine yields trifluoromethyl derivatives with high regioselectivity.
- Debarge, Sébastien,Violeau, Bruno,Bendaoud, Nohair,Jouannetaud, Marie-Paule,Jacquesy, Jean-Claude
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p. 1747 - 1750
(2007/10/03)
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- Process for preparing flunixin and intermediates thereof
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Process for preparing a key intermediate, 2-methyl-3-trifluoromethylaniline (MTA) of Flunixin, as well as novel intermediates thereof are described.
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- Process for preparing Flunixin and intermediates thereof
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Process for preparing a key intermediate, 2-methyl-3-trifluoromethylaniline (MTA) of Flunixin, as well as novel intermediates thereof are described.
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- Improved Process for the Preparation of 2-Methyl-3-trifluoromethylaniline: A Versatile Intermediate for Flunixin Synthesis
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A detailed new experimental investigation into the synthesis of Flunixin via 2-methyl-3-trifluoromethylaniline is described.The coupling process between 2-methyl-3-trifluoromethylaniline and 2-chloronicotinate was achieved stoichiometrically and in high yield, when ethylene glycol was used as reaction solvent at 160 deg C.
- Jaouhari, Rabih,Quinn, Philip
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p. 2243 - 2246
(2007/10/02)
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- Preparation of substituted anilino-nicotinic acid derivatives
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Substituted anilino-nicotinic acid derivatives are readily prepared from the condensation of two intermediates, 2-alkyl-3-perfluoroalkyl-anilines and alkyl 2-chloronicotinates. The 2-alkyl-3-perfluoroalkyl-aniline intermediate can be prepared via a novel three step synthesis. 3-Perfluoroalkyl-anilines are reacted with an amine directing protecting group reagent to protect the amine. The protected amine is then alkylated, and finally, the directing group is removed to form the 2-alkyl-3-perfluoroalkyl-aniline intermediate. The 2-alkyl-3-perfluoroalkyl-aniline intermediate is condensed with the alkyl 2-chloronicotinate to form the anilino-nicotinic acid derivative.
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- Synthesis of 3-amino-2-methylbenzotrifluoride
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This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride from benzotrifluoride. The process comprises nitrating benzotrifluoride to form 3-nitrobenzotrifluoride, reacting this compound with trimethyl sulphoxonium halide to form 3-nitro-2-methylbenzotrifluoride and reducing the nitro group to an amino group.
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- Novel synthesis of 3-amino-2-methylbenzotrifluoride from N-(2-X-5-trifluoromethylphenyl)-S,S-dimethylsulfimide
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This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride, and to certain novel intermediates produced by the process. 3-Amino-2-methylbenzotrifluoride is a key intermediate useful in the preparation of valuable therapeutic agents such as, for example, 2-(2-methyl-3-trifluoromethyl)anilino nicotinic acid.
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- 4- and 5-Substituted 2,3-dihydro-1H-isoindoles, pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
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Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using novel 2,3-dihydro-1H-isoindole compounds having 4- and 5-substituents.
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- Novel synthesis of 3-amino-2-methylbenzotrifluoride and the intermediates thereof
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This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride from 4-X-substituted-2-methylthiomethylbenzotrifluorides. The former compounds are useful in the preparation of anilino-nicotinic and anilino-anthranilic acids exhibiting analgesic, anti-inflammatory or anti-diarrheal properties. Some of the intermediates are novel per se.
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- Trifluoromethyl substituted 1-aminoindanes
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4(5 or 6 or 7)-Trifluoromethyl-1-aminoindanes, useful as inhibitors of N-methyl transferase.
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