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Application of fludioxonil carboxylic acid derivatives in plant vascular tissue targeting medicament

A vascular and tissue technology, applied in the field of application of fludioxonil carboxylic acid derivatives in plant vascular tissue targeting agents, achieving good control effects

Active Publication Date: 2021-04-06
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fludioxonil carboxylic acid derivatives have been used in medicine, as CRTH2 receptor antagonists (Chinese published patent CN 101072773 B), but fludioxonil carboxylic acid derivatives are used as banana fusarium wilt vascular tissue targeting fungicides. The effect has not been reported

Method used

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  • Application of fludioxonil carboxylic acid derivatives in plant vascular tissue targeting medicament
  • Application of fludioxonil carboxylic acid derivatives in plant vascular tissue targeting medicament
  • Application of fludioxonil carboxylic acid derivatives in plant vascular tissue targeting medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Chemical synthesis and structural identification of fludioxonil carboxylic acid derivatives 1a and 1b

[0024] Experimental method: such as figure 1 The synthetic route shown is that fludioxonil is dissolved in acetonitrile (CH 3 CN) solution, add cesium carbonate (Cs 2 CO 3 ) and tetrabutylammonium iodide (TBAI) and stirred at room temperature for 1 h. Then methyl bromoacetate was added dropwise, and the reaction bottle was moved to an oil bath and heated to 80°C with stirring. After the reaction of the raw materials is completed, add 1mol / L hydrochloric acid solution to adjust the reaction solution to acidity (pH=2), extract three times with ethyl acetate, and finally wash with saturated sodium chloride solution, concentrate under reduced pressure and separate by column chromatography Target compound 1b.

[0025] The target compound 1b was dissolved in tetrahydrofuran (THF) and water (H 2 O) In the mixed solution, add lithium hydroxide monohydrate (Li...

Embodiment 2

[0046] Embodiment 2: the conductance of the fludioxonil carboxylic acid derivative prepared in embodiment 1 in the phloem of the model plant castor bean seedling

[0047] Experimental method: Castor bean seedlings are model plants for the study of phloem transport, and are widely used to screen and evaluate the transport of pesticides in plant phloem.

[0048]The present embodiment adopts this method to carry out phloem conductance evaluation to the fludioxonil carboxylic acid derivative synthesized in embodiment 1, and concrete operation is as follows, castor bean cotyledon is immersed in the buffer solution containing 20mmol / LMES (pH 5.0), simultaneously Add the fludioxonil carboxylic acid derivatives (1a, 2a, 3a, 4a, 1b, 2b, 3b and 4b) at a final concentration of 0.1mmol / L to be tested, and after treating the castor leaves for 2 hours, cut the hypocotyls and collect them within 2 hours. Phloem fluid exuded from the incision. The collected phloem fluid was diluted with acet...

Embodiment 3

[0050] Example 3: Phloem transport properties of fludioxonil carboxylic acid derivative 1a at different apoplast pHs

[0051] Experimental method: castor cotyledon leaves are immersed in the buffer solution containing 20mmol / L MES (pH 5.0 and 6.0) or 20mmol / L HEPES (pH7.0 and 8.0), while adding the final concentration of 0.1mmol / L fludioxonil carboxylic acid to be tested For derivatives, after treating the castor cotyledons for 2 hours, cut the hypocotyls, and collect the phloem fluid exuded from the cuts within 2 hours. The collected phloem fluid was diluted with acetonitrile and analyzed by high performance liquid chromatography (HPLC). The experiment was repeated 3 times, each treatment had 4 seedlings and each plant was tested individually.

[0052] Experimental results: the results are as follows image 3 As shown, as the pH value of the culture medium increased, the concentration of fludioxonil carboxylic acid derivative 1a in the phloem gradually decreased, and the co...

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Abstract

The invention discloses an application of fludioxonil carboxylic acid derivatives in a plant vascular tissue targeting medicament. According to the invention, the non-systemic bactericide fludioxonil is subjected to carboxylic acid group modification, and the obtained fludioxonil carboxylic acid derivative shows good plant phloem conductivity, so that the fludioxonil carboxylic acid derivative can be used as a plant vascular tissue targeting bactericide. The fludioxonil carboxylic acid derivative disclosed by the invention shows a good prevention and treatment effect when being used for preventing and treating banana wilt.

Description

technical field [0001] The invention belongs to the technical field of pesticides, and in particular relates to the application of a class of fludioxonil carboxylic acid derivatives in plant vascular tissue targeting agents. Background technique [0002] As the main banana producing country in the world, China has reported banana wilt in all major banana producing areas in my country, which has brought a devastating blow to my country's banana industry and has become the most important factor restricting the development of my country's banana industry. Banana Fusarium wilt is a soil-borne vascular disease caused by Fusarium oxysporum f.sp.cubense (Foc). reproduce in large numbers. As a devastating plant disease, the control of banana wilt has always been a worldwide problem. Once the pathogen invades the banana vascular tissue, traditional fungicides cannot directly act on the pathogen, which is also the main reason why chemical control of banana wilt is difficult to be ef...

Claims

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Application Information

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IPC IPC(8): A01N43/36A01P3/00C07D405/04
CPCA01N43/36C07D405/04
Inventor 吴瀚翔徐汉虹姚光凯肖春霞
Owner SOUTH CHINA AGRI UNIV