Synthetic method of emamectin benzoate crude product

Abstract

The invention relates to a synthetic method of an emamectin benzoate crude product, which is characterized in that: avermectin B1a is used as an initial raw material, and is subjected to an oxidationreaction, an ammoniation reaction, a reduction reaction and a salification reaction to obtain the emamectin benzoate crude product, and the reactions are carried out in a reaction system using dimethylformamide, tetrahydrofuran or tetrahydropyrane as a reaction solvent. According to the invention, the abamectin B1a is directly used as an initial synthesis raw material; the emamectin benzoate is synthesized by adopting a four-step method instead of a six-step method, so that the synthesis process steps are simplified, the production period is shortened, the production cost advantage is obvious,only one reaction solvent is used in the whole synthesis process, the recycling is convenient, the discharge amount of byproducts is very low, and the environmental pollution is not easily caused.

Description

technical field [0001] The invention belongs to the technical field of antibiotic synthesis, in particular to a method for synthesizing crude emamectin emamectin by using abamectin B1a. Background technique [0002] Emamectin benzoate, also known as emamectin benzoate, is a high-efficiency, low-toxicity, low-residue, green and environment-friendly biological source insecticide developed and marketed by Novartis. Emamectin benzoate is a derivative of abamectin, a biological fermentation product, and its biological activity is higher than that of abamectin compared with the parent. Emamectin emamectin has a wide insecticidal spectrum, and has a good poisonous effect on cotton bollworm, beet armyworm, gray winged armyworm, tobacco armyworm, etc., especially for Lepidoptera pests, the insecticidal effect is excellent, It is widely used in cabbage, cabbage and other vegetables, soybeans, tobacco, rice and other crops and fruit trees. Therefore, the unique insecticidal mode of e...

AI Technical Summary

Problems solved by technology

[0007]1 takes avermectin as the initial raw material, and obtains formazan through synthetic steps such as hydroxyl protection, oxidation, ammoniation, hydrogenation reduction, deprotection reaction and salt-forming reaction. Crude vitamin salt, the synthetic route is more complicated

[0008]2 A variety of raw materials are involved in the synthesis of emamectin emamectin salt. Due to the high price and high consumption, the production cost of emamectin emamectin salt is high and the economic benefit is high. Low

[0009]3 This production process uses many kinds of organic reagents, and during the synthesis of emamectin emamectin salt, there are by-products discharged, which are easy to pollute the environment

[0010]4 The product yield is about 60%, which is relatively low

[0014]1 The product quality (49% purity) is poor, and the production yield (62%) is low

[0015]2 Many types of reaction solvents were used in the production process, which caused a certain impact on the environment

[0016]3 This method is only a test method and has not been verified in industrialized large-scale production. The feasibility and effectiveness of the method need to be further confirmed