Preparation method for carbazolyl isopropanolamine derivative and application thereof

A technology of carbazolyl isopropanolamine and alkyl, which is applied in the field of preparation of carbazolyl isopropanolamine derivatives, and can solve the problems of environmental pollution, poor prevention effect and high toxicity

Active Publication Date: 2019-04-16
GUIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing commercialized antimicrobial agents (such as eclopyrazole, thiazocopper, and ketal) not only have problems such as poor control effect, high toxicity, and serious environmental pollution, but also increase the drug resistance of pathogens. It is urgent to find highly effective antibacterial agents Active compounds of pathogenic bacteria, on this basis, create green new pesticides with independent intellectual property rights, and provide candidate drugs for the prevention and control of bacterial diseases of crops

Method used

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  • Preparation method for carbazolyl isopropanolamine derivative and application thereof
  • Preparation method for carbazolyl isopropanolamine derivative and application thereof
  • Preparation method for carbazolyl isopropanolamine derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Preparation of 1-(benzylamino)-3-(9H-carbazolyl)-2-hydroxypropanol

[0053] Add 9-(2-methyloxyethylene)-9H-carbazole (0.90mmol) and potassium carbonate (0.90mmol) into 5mL isopropanol solution dissolved with benzylamine (1.80mmol), and react at 60°C for 6 hours After stopping the reaction, desolvation, column chromatography (eluent CH 2 Cl 2 :CH 3 OH=200:1) to obtain a white solid with a yield of 53.7%.

[0054] The structures, H-NMR and C-NMR data of some synthesized compounds containing carbazolyl isopropanolamine structures are shown in Table 1, and their physical and chemical properties are shown in Table 2.

[0055] H NMR spectrum and carbon spectrum data of some compounds in Table 1

[0056]

[0057]

[0058]

[0059] Table 2 Physicochemical properties of some target compounds

[0060]

[0061]

[0062] Pharmacological Example 1:

[0063] The inhibitory rate of the target compounds to plant pathogenic bacteria was tested by turbidim...

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Abstract

The invention relates to a preparation method for carbazolyl isopropanolamine derivative and application thereof. The structure of the compound is shown in the formula (I), and the compound achieves the better effect of inhibiting xanthomonas oryzae, ralstonia solanacearum, cucumber xanthomonas oryzae, konjak xanthomonas oryzae, xanthomonas citri, grape ulcer bacteria, tomato ulcer bacteria, kiwifruit ulcer bacteria, apple ulcer bacteria, cucumber botrytis cinerea, chili blight bacteria, sclerotinia sclerotiorum, wheat gibberella saubinetii, potato late blight, blueberry root rotting bacteriaand the like.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a preparation method and application of a class of carbazolyl isopropanolamine derivatives. Background technique [0002] Plant-borne bacterial diseases are one of the most destructive plant diseases in the world, and even cause crop failure in severe cases, causing great harm to crops and economic crops in our country. Among them, bacterial diseases such as rice bacterial blight (Xanthomonas oryzae pv.oryzae, Xoo) and citrus canker (Xanthomonas axonopodispv.citri, Xac) cause losses of hundreds of millions of dollars to agriculture every year. Existing commercialized antimicrobial agents (such as eclopyrazole, thiazocopper, and ketal) not only have problems such as poor control effect, high toxicity, and serious environmental pollution, but also increase the drug resistance of pathogens. It is urgent to find highly effective antibacterial agents Active compounds of p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/86C07D405/12C07D409/12A01N43/38A01P1/00A01P3/00
CPCA01N43/38C07D209/86C07D405/12C07D409/12
Inventor 杨松赵永亮王培义黄星龙青素吴元元薛伟
Owner GUIZHOU UNIV
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