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Isothiazole-o-pyrimidone compound and application thereof

A kind of technology of pyrimidinone and compound, applied in the field of isothiazolopyrimidone compound, can solve the problem that structure isothiazolopyrimidone compound has not been reported and the like

Active Publication Date: 2013-09-11
SHENYANG SINOCHEM AGROCHEMICALS R&D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In the prior art, the structure of the isothiazolopyrimidinone compound shown in the general formula I of the present invention has not been reported

Method used

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  • Isothiazole-o-pyrimidone compound and application thereof
  • Isothiazole-o-pyrimidone compound and application thereof
  • Isothiazole-o-pyrimidone compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Example 1: Preparation of compound 160

[0122]

[0123] 1) Preparation of intermediate 4-amino-3-phenyl-5-isothiazole ethyl ester (II-1)

[0124] (1) Preparation of benzoyl nitrile oxime sodium salt

[0125] Weigh 8.15 g (0.20 mol) of sodium hydroxide and 23.41 g (0.20 mol) of benzyl cyanide into a 1000 ml three-necked flask equipped with mechanical stirring, thermometer and exhaust gas absorption device, add 150 ml of absolute ethanol, and cool to 10-20°C. At this temperature, a solution of 28.11 g (0.24 mol) of isoamyl nitrite in 50 ml of absolute ethanol was slowly added dropwise. After the addition, the ice bath was removed, and the reaction was continued for 2.5 hours at room temperature. After the reaction was monitored by TLC, 200ml of ether was added to the reaction solution, stirred for 30 minutes and filtered, the filter cake was washed with ether, dried in air and vacuum (70-80℃) to obtain 15.31 g of white solid, melting point: 286-288 ℃.

[0126] (2) Preparatio...

Embodiment 2

[0148] Example 2: 30% compound 7 wettable powder

[0149]

[0150] The compound 7 and other components are fully mixed and pulverized by an ultrafine pulverizer to obtain a 30% wettable powder product.

Embodiment 3

[0151] Example 3: 30% compound 48 wettable powder

[0152]

[0153] The compound 48 and other components are fully mixed and pulverized by an ultrafine pulverizer to obtain a 30% wettable powder product.

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Abstract

The invention discloses an isothiazole-o-pyrimidone compound. The compound has the structure shown in the general formula I, wherein each substituent group is defined in the specification. The compound with the general formula I has high activity on multiple pathogenic bacteria in the agricultural field and particularly has a good effect of preventing and treating rice blast, cucumber downy mildew, cucumber gray mold and puccinia polysra under low dose; moreover, the compound also has high insecticidal activity. Therefore, the invention comprises application of the compound which is shown in the general formula I and serves as a fungicide and a pesticide in the fields of agriculture and the like.

Description

Technical field [0001] The invention belongs to the field of agricultural sterilization and pesticides. Specifically, it relates to an isothiazolopyrimidinone compound and its use. Background technique [0002] As fungicides and insecticides are used for a period of time, germs and pests will develop resistance to them, so it is necessary to continuously develop new and improved compounds and compositions with fungicidal and insecticidal activities. At the same time, with people's increasing demand for agricultural and livestock products and increasing attention to environmental protection, there has always been a need to use new low-cost, environmentally friendly sterilization and pesticides. [0003] Patent US4539328A relates to compounds of the following general formula as nematicides: [0004] [0005] Among them: A is selected from hydroxyl, alkoxy, benzyloxy, NHR; R is selected from hydrogen, alkyl, CH 2 CH 3 OH, CH 2 CH 2 OCOCH 3 ; Z is selected from hydrogen, halogen, alkyl...

Claims

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Application Information

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IPC IPC(8): C07D513/04A01N43/90A01P3/00A01P7/04
Inventor 康卓张静孙芹关爱莹梁博李淼王军锋宋玉泉刘长令
Owner SHENYANG SINOCHEM AGROCHEMICALS R&D CO LTD
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