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Preparation method of trifluoromethyl tetralone compound

A technology of trifluoromethyltetralone and fluoromethyltetralone, which is applied in the field of preparation of trifluoromethyltetralone compounds, can solve the problems of large side effects, increased burden on the gastrointestinal tract, and slow curative effect, and achieves The effect of low cost, remarkable bactericidal and bacteriostatic effects, and simple preparation method

Pending Publication Date: 2020-06-26
上海孜岚医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The preparation method of a trifluoromethyltetralone compound proposed by the present invention solves the problems of slow curative effect, large side effects, and increased burden on the gastrointestinal tract

Method used

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  • Preparation method of trifluoromethyl tetralone compound
  • Preparation method of trifluoromethyl tetralone compound
  • Preparation method of trifluoromethyl tetralone compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] A preparation method of trifluoromethyl tetralinone compound, comprising the following steps:

[0031] S1. Take 17.61g (0.1mol) of 4-methoxytetralone and add it to a 250mL three-neck flask, then add 100Ml dichloromethane into it, add 28.21g (0.1mol) of trifluoromethanesulfonic anhydride under ice bath, and keep warm for 2h , quenched the reaction with saturated ammonium chloride, extracted with dichloromethane, and dried over anhydrous sodium sulfate to obtain product S215g, with a yield of 50.0%. Other products can be obtained in the same way.

[0032]S2. Take 31.01g (0.1mol) of S2 and put it into a 250mL three-necked flask, then add 100ml of acetonitrile into it, add 22.82g (0.1mol) of ammonium persulfate in the ice bath, react in the ice bath for 30min, remove the ice bath, and continue to stir for 2h , the reaction was monitored by TLC, the reaction was quenched with saturated ammonium chloride, extracted with dichloromethane, and dried over anhydrous sodium sulfat...

Embodiment 2

[0041] A preparation method of trifluoromethyl tetralinone compound, comprising the following steps:

[0042] S1. Take 16.1g (0.1mol) of 4-methyltetralone and add it into a 250mL three-neck flask, then add 100ml of dichloromethane, add 28.21g (0.1mol) of trifluoromethanesulfonic anhydride under ice bath, and keep it warm for 2h. The reaction was quenched with saturated ammonium chloride, extracted with dichloromethane, and dried over anhydrous sodium sulfate to obtain 13.2 g of product S21 with a yield of 45.2%.

[0043] S2. Take 29.2g (0.1mol) of S21 and add it to a 250mL three-necked flask, then add 100ml of acetonitrile into it, add 22.82g (0.1mol) of ammonium persulfate in the ice bath, react in the ice bath for 30min, remove the ice bath, and continue stirring for 2h , the reaction was monitored by TLC, quenched with saturated ammonium chloride, extracted with dichloromethane, and dried over anhydrous sodium sulfate to obtain product S35.72g, yield 25.3%.

[0044] S3. Ta...

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PUM

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a trifluoromethyl tetralone compound. The problem that a large number of widely applied antibiotics have resistance so that serious side effects and heavy economic pressure are caused on patients due to excessive and excessive use of antibiotics in the prior art is solved. The structuralgeneral formula of the compound is shown in the specification, wherein R1, R2, R3, R4, X and Y are defined in the claim 1, and R1, R2, R3 and R4 are the same or different. The compound provided by theinvention has significant bactericidal and bacteriostatic effects, is suitable for the fields of medicines and farm chemicals, solves the problems of excessive use and excessive use of antibiotics caused by resistance of a large amount of antibiotics in the prior art, and is worthy of further development.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for preparing trifluoromethyltetralone compounds. Background technique [0002] In recent years, due to the more and more frequent application of antibiotics, the birth of various superbugs has caused enormous pressure on medical workers and the people, making the research and development of new antibiotics urgent. [0003] However, a large number of antibiotics that are widely used now have resistance, resulting in the excessive and excessive use of antibiotics, causing serious side effects and heavy economic pressure on patients. Based on the excellent biological activity of nitrogen heterocycles, especially in terms of bactericidal and bacteriostatic performance, we used a series of classic chemical synthesis techniques to design tetralin compounds containing trifluoromethyl groups, and at the same time carried out preliminary research on their biological activities ...

Claims

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Application Information

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IPC IPC(8): C07D401/04C07D401/14A01N43/56A01P3/00A61P31/04
CPCC07D401/04C07D401/14A01N43/56A61P31/04
Inventor 谢如良吴鲁豫
Owner 上海孜岚医药科技有限公司
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