Process for preparing 2-amino-4'-fluoro-benzophenone

A technology of benzophenone and fluorobenzoyl benzoic acid is applied in the field of preparation of 2-amino-4'-fluoro-benzophenone, and can solve the problem of harsh reaction conditions, long reaction steps, and side-by-side reactions. Over-reacting issues

Inactive Publication Date: 2005-11-02
庄罗元
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Problems solved by technology

[0007] Among the above three preparation methods, the first method will use Grignard reagent and butyllithium, the reaction conditions are harsh, the operation requirements are strict, the industrial production is difficult, and the yield is 41.2%; Many, the yield also only has 44%; The reaction step of the third method is long, always only has yield 49%

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  • Process for preparing 2-amino-4'-fluoro-benzophenone
  • Process for preparing 2-amino-4'-fluoro-benzophenone

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Embodiment Construction

[0020] The following examples illustrate the specific implementation method of the present invention

[0021] The first step: the preparation of 2-p-fluorobenzoylbenzoic acid

[0022] Add 25g (0.17mol) of phthalic anhydride and 50g (0.375mol) of anhydrous aluminum trichloride to 120g (1.25mol) of fluorobenzene, the reaction occurs immediately, and hydrogen chloride gas is released, which is absorbed by water. At this time, the reaction liquid is Orange yellow, slowly heated to 55°C-70°C, the reaction proceeds violently, the reaction solution gradually turns dark red, keep warm for 4 hours, cool to room temperature, slowly pour the reaction solution into ice water filled with hydrochloric acid while stirring, and put The reaction solution was adjusted to PH1, the organic layer was separated, washed with water, the excess fluorobenzene was recovered under reduced pressure, cooled to room temperature, a large amount of solids were precipitated, 40 g of white powder was obtained a...

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Abstract

The present invention discloses the preparation process of 2-amino-4'-fluoro-diphenylketone. Phthalic anhydride as material is first Friedel-Crafts reacted with fluorobenzene to obtain 2-p-fluorobenzene formyl benzoic acid; 2-p-fluoro benzoyl benzoic acid is then acyl chlorinated and amidated to obtain 2-p-fluorobenzene formyl benzoyl benzamide; and 2-p-fluorobenzene formyl benzoyl benzamide is finally Hofmann degraded to obtain 2-amino-4'-fluoro-diphenylketone. The present invention has optimized reaction condition and total yield over 78.6 %.

Description

Technical field: [0001] The invention relates to a preparation method of 2-amino-4'-fluoro-benzophenone. Background technique: [0002] 2-Amino-4'-fluoro-benzophenone is an intermediate used in the production of ITAVASTATIN, which is an intermediate in the preparation of anti cholesterol drugs. [0003] At present, there are three synthetic methods for the preparation of 2-amino-4'-fluoro-benzophenone: [0004] The first is made from isatoic anhydride, which is first reacted with methoxymethylamine, then Grignard reaction with p-fluorobromobenzene, and then rearranged with butyllithium; [0005] The second is made by isatoic anhydride as raw material, which first reacts with thionyl chloride to generate o-chloroformylphenyl isocyanate, and then reacts with fluorobenzene to obtain it; [0006] The third is to use anthranilic acid as the raw material, first protect the amino group with p-toluenesulfonyl chloride, then chlorinate to obtain the acid chloride, and then carry ou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C225/22
Inventor 庄罗元
Owner 庄罗元
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