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Method for preparing emamectin benzoate

A technology of emamectin salt and methylamino group, applied in the field of optimization research of emamectin salt production method, can solve problems such as unfavorable large-scale production, and achieve the effects of improving yield, easy purification and high selectivity

Inactive Publication Date: 2016-06-01
BEIHAI GOFAR MARINE BIOLOGICAL IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because tetrakis (triphenylphosphine) palladium is extremely unstable, it needs to be used and made now, so this synthetic route is not conducive to large-scale production

Method used

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  • Method for preparing emamectin benzoate
  • Method for preparing emamectin benzoate
  • Method for preparing emamectin benzoate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 15

[0026] Embodiment 15-position hydroxyl protection, 4 "-position hydroxyl oxidation

[0027] Add 10g of Abamectin and 50ml of dichloromethane into a three-necked flask with a condenser tube and a thermometer, stir to make it dissolve completely, then add triethylamine and dimethylmethylene containing 50% p-methoxyphenol methyl chloride 30ml of sulfone, heated to 60±2°C, kept warm for 3h, then concentrated, lowered to room temperature, and left for the next reaction.

Embodiment 2

[0028] Embodiment 2 ammoniation reduction reaction

[0029] Add 80ml of methylaminoalcohol solution to the concentrated solution of Example 1, then add 0.05mg of manganese catalyst, heat up to 85±2°C, keep warm for 4h, and obtain 5-O-protecting group-4″-methylamino - The reaction solution of Abamectin was directly used for the next reaction without processing.

Embodiment 3

[0030] Embodiment 3 deprotection reaction

[0031] Add hydrochloric acid to the reaction solution containing 5-O-protecting group-4″-methylamino-abamectin, adjust the pH to 2-3, DDQ0.5g, raise the temperature to 110±2°C, and the reaction time is 4h , Obtain 4 "-methylamino-abamectin solution.

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Abstract

The invention provides a method for prepating emamectin benzoate. The method comprises four steps: a 5-hydroxyl protection and 4''-hydroxyl oxidation reaction, an aminoation-reduction, a deprotection reaction and a salt forming reaction, wherein 5-hydroxyl protection selects a protective agent which is selected from p-methoxyphenol methyl, p-methoxybenzyl, p-methoxyphenol methyl chloride, 2-(trimethylsilyl)ethoxycarbonyl, dimethoxy benzoyl methane, chloromethyl 2-ethyl ether and 2-(trimethylsilyl)ethloxymethyl. The method overcomes generation of a by-product by a reaction intermediate, so that yield and purity of the product are greatly increased, purification is easy, and the method has the characteristics of easy control of the production process, high yield and environmental protection.

Description

technical field [0001] The invention belongs to the field of preparation of pesticide raw materials, and in particular relates to the optimization research of a production method of emamectin benzoate. Background technique [0002] Emamectin Benzoate, also known as emamectin benzoate, its chemical name is 4″-methylamino-4”-deoxyabamectin B1 benzoate, which is based on fermentation products A new type of high-efficiency semi-synthetic antibiotic insecticide and acaricide biopesticide developed by Abamectin B1. Its mechanism of action is to interfere with the neurophysiological activities of insects, stimulate the release of γ-aminobutyric acid, and inhibit the conduction of nerve impulses in insects . Emamectin benzoate is a high-efficiency, low-toxicity, low-residue, green and environment-friendly biological source insecticide developed and marketed by Novartis. Its structure modification is based on avermectin, and methylamine is introduced at the 4″-position It is the mo...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/00
Inventor 陈书勤黄巧萍李有志孟宪福张敦河龙先进
Owner BEIHAI GOFAR MARINE BIOLOGICAL IND CO LTD
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