Compound, preparation method and antibacterial application thereof

A technology of compounds and bacteriostats, applied in the field of compounds and their preparation, to achieve the effect of less raw materials

Inactive Publication Date: 2016-03-23
ZHONGKAI UNIV OF AGRI & ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is reported that carbendazim and indole acetic acid are used together in pharmaceuticals, the effects

Method used

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  • Compound, preparation method and antibacterial application thereof
  • Compound, preparation method and antibacterial application thereof
  • Compound, preparation method and antibacterial application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 formula (I) compound

[0037]

[0038] Add 10 mmol of indole acetic acid (II), 10 mmol of N,N'-dicyclohexylcarbodiimide (DCC), a catalytic amount of 4-dimethylaminopyridine (DMAP) and 12 mmol of bromoethanol (III) to 30 mL of dichloromethane , stirred at room temperature for 2h. After completion of the reaction, add a large amount of water to extract, concentrate, and column chromatography to obtain a colorless intermediate compound (IV).

[0039]

[0040] Add 5mmol of carbendazim (V) to 20mL of dimethylformamide, stir at room temperature, add 7.5mmol of cesium carbonate, stir for 30min, cool down to 0°C, and dropwise add 6mmol of intermediate compound (IV) in N , N-dimethylformamide (DMF) solution 30mL, slowly warming up to room temperature, stirring for 36h. After the reaction was completed, the pH value was adjusted to neutral with 3mol / L HCl solution, extracted with ethyl acetate, and column chromatography was used to obtain t...

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PUM

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Abstract

The invention relates to a preparation method of a novel medicine for inhibiting Cylindrocladium parasiticum, Colletotrichum corda and Phomopsis(Sacc.)Bubak. Indoleacetic acid, bromoethanol and carbendazim active compounds are used as synthetic raw materials to prepare an indoleacetic acid-carbendazim conjugate, which is the finish product, through a reaction. The invention also discloses nuclear magnetic resonance structure data, a hydrogen spectrogram and a carbon spectrogram of the novel compound. The compound has excellent antibacterial effects on the Cylindrocladium parasiticum, the Colletotrichum corda and the Phomopsis(Sacc.)Bubak.

Description

technical field [0001] The invention belongs to the field of pesticides, and in particular relates to a compound and its preparation method and application. Background technique [0002] Due to the broad spectrum of carbendazim, it has a certain inhibitory effect on peanut black rot, anthracnose and Phomopsis. Anthracnose fungus (Colletotrichum Corda) is a worldwide plant pathogen, which can cause a variety of plant diseases and cause great economic losses to crops, especially in tropical and subtropical regions. Among them, the host range of glyosporium anthracnose is wide, and it can cause diseases in various crops such as citrus, coffee, mango, papaya and so on. The prevention and control of anthracnose mostly focuses on the use of triadimefon and benzimidazoles, but studies have shown that the glyospora anthracnose of mango anthracnose and camellia oleifera anthracnose has been treated with benzimidazole fungicides such as carbendazim, Resistance to thiophanate-methyl ...

Claims

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Application Information

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IPC IPC(8): C07D403/12A01N43/52A01P3/00
CPCA01N43/52C07D403/12
Inventor 杨静美郑奕雄雷泽湘
Owner ZHONGKAI UNIV OF AGRI & ENG
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