A kind of 4-fluoro substituted arylamine compound and its synthetic method

A technology for aniline compounds and synthesis methods, which is applied to the preparation of amino compounds, the preparation of amino hydroxy compounds, chemical instruments and methods, etc., can solve the problems of expensive reagents, unsuitable for scale-up production, etc. Lipophilic effect

Active Publication Date: 2022-06-03
江苏笃行致远新材料科技有限公司
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Problems solved by technology

[0012] Literature Nature 2015,524,208-211 reported the use of aryl bromide, AgF and KF as a fluorine source under the catalysis of palladium for fluorination. This method is not suitable for scale-up due to the use of an air- and water-sensitive catalytic system, and the reagent is expensive. Production

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  • A kind of 4-fluoro substituted arylamine compound and its synthetic method
  • A kind of 4-fluoro substituted arylamine compound and its synthetic method
  • A kind of 4-fluoro substituted arylamine compound and its synthetic method

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Abstract

The invention discloses a method for synthesizing 4-fluorine-substituted arylamine compounds, which comprises the following steps: 1) taking acyl-protected phenylhydroxylamine as a substrate, and using sulfonyl fluoride as a fluorine source in a polar solvent, Generating 4-fluoro-substituted aniline compounds under basic conditions; 2) deprotecting groups under dilute acidic conditions or catalytic hydrogenation of Pd to obtain the 4-fluoro-substituted arylamine compounds. The synthetic 4-fluorine-substituted aniline compound of the present invention can be widely used in the preparation of fluorine-containing medicines, pesticides and dye intermediates because the introduction of fluorine atoms greatly increases its lipophilicity; meanwhile, the raw materials used in the present invention All are industrial products, cheap and easy to get, and are commercially available; the yield of 4-fluoroarylaniline prepared by the present invention is high, and a product with a purity of ≥99% can be obtained with a yield greater than 90%; the present invention is simple to operate , the low-cost process is very suitable for industrialization and can be widely used.

Description

A kind of 4-fluoro-substituted arylamine compound and synthetic method thereof technical field The invention belongs to the technical field of fine chemical industry, relate to the technical field of organic synthesis, particularly a kind of 4-fluorine substitution Arylamine compounds and synthetic methods thereof. Background technique Since fluorine is the most electronegative element, the introduction of fluorine atoms makes fluorine-containing organic compounds have a unique Physical properties, chemical properties and physiological activities make fluorine-containing organic compounds have chemical stability, surface activity and excellent Temperature resistance and other characteristics. Therefore, in many cutting-edge technologies and major industrial projects, as well as in pharmaceuticals, pesticides and other industries, fluorine-containing Compounds have been extensively and deeply researched and applied. Arylaniline substituted by p-fluorine is widely p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C209/62C07C211/52C07C213/02C07C217/84C07C319/20C07C323/36C07C315/04C07C317/36
CPCC07C209/62C07C211/52C07C231/10C07C269/06C07C213/02C07C217/84C07C319/20C07C323/36C07C315/04C07C317/36C07C233/15C07C271/28C07C233/25C07C233/43C07C323/41C07C317/40Y02P20/55
Inventor 刘文娟刘智慧崔志鹏崔晓雷田瑞芳
Owner 江苏笃行致远新材料科技有限公司
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