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92 results about "Milbemycin" patented technology

The milbemycins are a group of macrolides chemically related to the avermectins and were first isolated in 1972 from Streptomyces hygroscopicus. They are used in veterinary medicine as antiparasitic agents against worms, ticks and fleas.

Preparation method of milbemycin oxime

The invention provides a preparation method of milbemycin oxime. The preparation method of milbemycin oxime comprises the following steps: extracting milbemycins, namely taking milbe mycelia obtained through fermentation as a raw material, extracting, concentrating, extracting, concentrating, extracting again and concentrating again, so as to obtain milbemycin; preparing milbemycin ketone, namely taking the milbemycin as a raw material, establishing an oxidation reaction system, after reaction is finished, filtering, concentrating, extracting and concentrating the reaction system, so as to obtain an intermediate product milbemycin ketone; synthesizing milbemycin oxime, namely dissolving milbemycin ketone with methanol and dioxane, dropwise adding hydroxylamine hydrochloride solution and reacting, concentrating the reaction system, extracting, drying and concentrating, so as to obtain a milbemycin oxime crude product; and purifying milbemycin oxime, namely crystallizing the milbemycin oxime crude product with a mixed solvent of trichloromethane and normal heptane, dissolving a crystalline product with ethanol, dropwise adding into water while stirring for carrying out crystallization, filtering, and drying, so that the milbemycin oxime finished product is obtained. The preparation method of the milbemycin oxime has the advantages that productivity is greatly improved, and cost is obviously reduced, so that the preparation method provided by the invention is obviously better than an existing preparation method.
Owner:HUBEI HONCH PHARMA

Synthetic method for milbemycin oxime

The invention provides a synthetic method for milbemycin oxime. The method comprises the following steps that 1, an oxidation reaction is performed, wherein milbemycins is used as raw materials, pypocholoride or chlorite is used as an oxidizing agent, piperidines free radical of nitroxide is used as a catalyst, a halide is used as a promoter, all the materials are subjected to the reaction in a dichloromethane solvent at the temperature being minus 5-15 DEG C for 0.5-4 h, and postprocessing is performed on a reaction product to obtain an intermediate product of milbemycin ketone; 2, an oximation reaction is performed, wherein methyl alcohol and 1,4-dioxane are used as a reactive solvent, hydroxylamine hydrochloride is used as an oximation reagent, the reaction is performed at the temperature being 25-35 DEG C for 10-16 h, and postprocessing and purification are performed to obtain milbemycin oxime. According to the method, industrial production of the milbemycin oxime is achieved in China for the first time, and the yield of the obtained product is higher than that of similar products both at home and abroad. Due to the fact that the pypocholoride is used as the oxidizing agent, pyridine nitroxide free radical is used as a catalyst, conditions are mild, few side reactions exist, the yield is high, and the cost is low.
Owner:HUBEI HONCH PHARMA
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