Novel methylamino abamectin benzoate ointment and production method thereof

Abstract

The invention relates to a methylamino abamectin benzoate ointment and a production method thereof. The ointment comprises the components, by mass, 10-25% of methylamino abamectin benzoate, 0.1-0.3% of antioxidants, 5-10% of cosolvent, 54.7-79.9% of sec-butyl acetate and 5-10% of other components. The key of the production method of the ointment is that sec-butyl acetate serves as a solvent of an amination reaction, a C-4 reduction reaction and a deprotection reaction during production of the ointment, excessive benzoic acid is added after methylamino abamectin is formed, the antioxidants and the cosolvent are added after salifying is achieved and moisture is concentrated to lower than 0.1%, and a final ointment product is obtained. Compared with an ordinary emamectin benzoate production process, the process reduces using amount of a reaction solvent, simplifies production steps and improves product yield. The production method provides a stable solvent system for methylamino abamectin benzoate, enables a processing process of a downstream preparation to be simple, safe and environment-friendly, can reduce 15%-20% of solvent cost, and has strong market popularization.

Description

technical field [0001] The invention relates to an emamectin benzoate ointment and a production method thereof. Background technique [0002] Emamectin benzoate is a high-efficiency semi-synthetic antibiotic insecticide synthesized from the fermented product abamectin. It has the characteristics of ultra-high efficiency, low toxicity, no residue, and no pollution. Compared with avermectin, the insecticidal activity is firstly improved, and it has a very good effect at a very low dose, and it does not harm beneficial insects in the process of controlling pests, which is conducive to the comprehensive control of pests and expands the insecticidal spectrum. , reducing the toxicity to humans and animals. The original drug of emamectin benzoate is white or light yellow crystalline powder with average stability. [0003] At present, the synthesis of emamectin benzoate starts from the component of avermectin B1, and the process is mainly divided into five steps, namely C-5 protec...

AI Technical Summary

Problems solved by technology

The disadvantage of this process is that the amount of reaction solvent used is large, and the degradation and unnecessary loss of emamectin benzoate will be caused due to the long time, high temperature and cumbersome steps in the drying and crushing process

[0004] More than 90% of the dosage forms of emamectin benzoate terminal use are emulsifiable concentrates and microemulsions. The longest solvents used in the preparation process are toluene and xylene. Toxic solvents will cause secondary pollution to farmland, and the hazards to users

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