Method for producing 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide

A technology of trifluoromethanesulfonyl and benzenesulfonamide, applied in chemical instruments and methods, preparation of organic compounds, organic chemistry, etc., can solve problems such as high price of trifluoroiodomethane, harsh reaction conditions, and low reaction yield , to achieve broad commercial application prospects, mild and controllable reaction conditions, and high reaction yield
CN109851535AInactive Publication Date: 2019-06-07TIANJIN MODERN VOCATIONAL TECH COLLEGE
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN MODERN VOCATIONAL TECH COLLEGE
Publication Date
2019-06-07
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The invention provides a method for producing 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide. 2-nitroaniline is used as an initial raw material, is subjected to diazotization reaction, trifluoromethyl sulfonation reaction, fluoronation, chlorosulfonation reaction, and is reacted with ammonium hydroxide to finally produce the 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide. Comparedwith reported synthesis methods, the method for producing the 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide has the advantages that the reaction yield of the synthesis route is high, used reaction agents are economic and easy to obtain, reaction conditions are mild and controllable, and in a reaction process, column chromatography and purification are not needed, so that the method for producing the 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide has wide commercial application prospects.
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Description

technical field

[0001] The invention belongs to the technical field of medicines, and in particular relates to a method for preparing 4-fluoro-3-(trifluoromethanesulfonyl)benzenesulfonamide. Background technique

[0002] Apoptosis is an evolutionarily conserved programmed cell death method, and its apoptosis process is very important for the generation, development and drug resistance of tumor cells. Therefore, tumor cells can be inhibited and eliminated by inducing tumor cell apoptosis. Wherein, Navitoclax (ATB-263) is one of potential medicines for the treatment of aging diseases, and the synthesis of Navitoclax (ATB-263) involves the fluoride intermediate 4-fluoro-3-(trifluoromethanesulfonyl)benzenesulfonamide (I ) preparation.

[0003] The preparation route of this key intermediate mainly consists of the following types:

[0004] (Synthetic Route 1): Using 2-fluorothiophenol as the starting material, trifluoromethylation in the presence of trifluoroiodomethane, and th...

Claims

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