Method for preparing high-purity moxidectin

Abstract

The invention relates to a method for preparing high-purity Moxidectin, which comprises the following steps: (1) macroporous absorption resin chromatography is carried out on Moxidectin solution which is purified in advance, the obtained product is eluted by the mixed solution of polar organic solvent and water; (2) the eluent is extracted by methylene dichloride, and then solvent is removed by conventional concentration; (3) protective reaction is carried out on the condensate to obtain upper protective liquid; (4) macroporous absorption resin chromatography is carried out on the upper protective liquid, and the chromatography is eluted by the mixed solution of the polar organic solvent and the water; (5) the eluted upper protective liquid is oxidized, and then deprotection and oximationreaction are carried out to obtain the reaction liquid of the Moxidectin; (6) macroporous absorption resin chromatography is carried out on the reaction liquid of the Moxidectin, and the chromatography is eluted by the mixed solution of the polar organic solvent and the water, so that the obtained eluent is the high-purity Moxidectin solution; the product can be separated out of the solution by using the conventional concentration and crystallization technology if necessary. As the macroporous absorption resin chromatography is used for separating instead of silica gel chromatography, the method is not only stable and controllable as well as is easy to industrialize, but also improves the product purity, the quality and the yield.

Description

technical field The invention relates to the field of medicinal chemistry, in particular, the invention relates to a method for preparing high-purity moxictine. Background technique The invention relates to a method for preparing moxictine. Moxidectin (INN: Moxidectin) is an agricultural antibiotic of macrolides, mainly used to treat parasitic diseases in animals such as cattle and sheep, and can be fermented by Streptomyces to produce Nemadectin (INN: Nemadectin) , and then obtained by chemical reaction. U.S. Patent No. 4,916,154A (its entire content is hereby incorporated as a reference) provides a method for preparing moxictine, that is, the fermented liquid produced after the fermentation of Streptomyces is separated from solid and liquid, and the nemoxictine solution obtained after leaching is passed through Extraction, silica gel column chromatography, gel chromatography to obtain nimoctine with a purity of more than 90% (HPLC), the purified nimoctine is passed throu...

AI Technical Summary

Problems solved by technology

This method can obtain the moxictine of purity more than 90%, but this method process is complicated, needs to operate and control all loaded down with trivial details silica gel chromatography, and this chromatographic solvent consumption is bigger, has no effect on the upper column thing that enters silica gel column High water requirements and low reusability lead to lower yields and higher costs for this chromatography

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