Preparation and application of bixafen derivatives

A technology of bixafen and derivatives, applied in the field of preparation and bactericidal activity of bixafen derivatives, to achieve good bactericidal activity, good water solubility and disease resistance activity, and the effect of preventing plant pathogens from invading

Inactive Publication Date: 2018-09-28
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Very hydrophilic drugs cannot pass through the lipid layer of the biomembrane, while very hydrophobic drugs remain as part of the biomembrane for similar and compatible reasons, so they cannot effectively enter the inner cytoplasm

Method used

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  • Preparation and application of bixafen derivatives
  • Preparation and application of bixafen derivatives
  • Preparation and application of bixafen derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0033] The following examples and bioassay results can be used to further illustrate the prevention of plant pathogens by the compounds of the present invention, but are not meant to limit the present invention.

[0034] Synthetic example

[0035] Preparation of target compound

[0036] 1. The synthesis of the general formula I shown in the present invention ----- taking TM-3 as an example

[0037]Add 0.12g (2.9mmol) of 60% sodium hydride and 20mL of dehydrated tetrahydrofuran into a 50mL round bottom flask, stir at room temperature for 10min, the system is a white turbid liquid. Add 1.0 g (2.4 mmol) of the prepared Bixafen (Bixafen) in 5 mL of tetrahydrofuran solution dropwise, a large number of bubbles are generated immediately, and continue to stir at room temperature for 20 min after the addition is complete. Then a solution of 0.47 g (2.9 mmol) of N,N-diisopropyl-2-chloroethylamine in 5 mL of tetrahydrofuran was added dropwise, and a catalytic amount of potassium iodide...

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Abstract

The invention relates to bixafen type derivatives with broad spectrum bactericidal activity and salts thereof, which are as shown in general formulas (I and II), wherein X represents oxygen atom, nitrogen atom and sulfur atom; n=0, 1, 2, 3, 4, 5...or (CH2)n represents alkyl with a branched chain; Y represents Cl<->, Br<->, F<->, I<->, AcO<->, acetylsalicylic acid radical, citric acid radical, salicylic acid radical, p-toluenesulfonic acid radical, sulfuric acid hydrogen radical or other negative ions. R1 represents the alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, alkenyl of 1-6 carbon atoms or aryl; R2 represents the alky of 1-6 carbon atoms, the alkoxy of 1-6 carbon atoms, the alkenyl of 1-6 carbon atoms or the aryl; or R1 and R2 are selected from the following structures.

Description

technical field [0001] The invention relates to the preparation and bactericidal activity of bixafen derivatives. Background technique [0002] Amide compounds are an important class of compounds with fungicidal activity. Since the first amide fungicide carboxin was successfully developed and marketed by Lilailu Company (now Kejuya Company) in 1966, the synthesis and bactericidal activity research of amide compounds has always been an important issue in the field of pesticides and even medicine. A research hotspot, there are a large number of amide compounds and varieties with novel structures reported. Since Knott discovered that antipyrine containing a pyrazole ring has analgesic, anti-inflammatory and antipyretic effects in 1883 and Thampson reported that 2-pyrazol-5-one can inhibit crop growth in 1946, pyrazole compounds have been used for their high efficiency. The biological activity has attracted the attention of the pesticide industry. Pyrazole carboxamide compoun...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C07D231/14A01N43/84A01N43/56A01P3/00
Inventor邹小毛丁会娟单鹏程刘俊傅翠蓉黄纯杨亚喆王鑫
OwnerNANKAI UNIV