Preparation method for methoxyl benzyl ester

Abstract

The invention provides a preparation method of methoxybenzyl, which uses penicillin and saturated salt water containing hydric sulphate. The invention uses penicillin as raw material to obtain penicillin sulfoxide via oxidization, to obtain penicillin sulfoxide ester via esterification, to be reacted with benzene sulfinate, to open ring and generate nitrogen heterocyclic butanone sulfinic acid intermediate, and electrolyzes the saturated salt water containing hydric sulphate, to utilize generated chlorizating agent to chlorizate the intermediate, at last ammonolyzes and closes ring to generate GCLE. The invention has the advantages of high product yield, high purity, low cost, and high quality, which uses electrolysis close-ring to process chlorization in production to assure safe reaction.

Description

technical field [0001] The invention relates to a method for preparing chemical raw materials, in particular to a method for preparing methoxybenzyl ester. Background technique [0002] 7-Phenylacetamide-3-Chloromethylcephlenoic Acid p-Methoxybenzyl Ester (GCLE for short) is a pharmaceutical intermediate, especially used to synthesize cephalosporin antibiotics. At present, a small number of domestic manufacturers have produced it in small quantities. GCLE, but there are still problems in the production process, the production cost is high, and the product quality is poor. In its synthesis in China, penicillin potassium salt is mainly used as raw material, which is obtained through esterification, oxidation, ring expansion, reduction and chlorine gas, and the key final chlorine Chlorization reaction can be synthesized by chlorine gas method and tert-butyl hypochlorite method, but the danger of using chlorine gas in chlorine gas method is strong, and the tert-butyl hypochlorit...

AI Technical Summary

Problems solved by technology

[0002] 7-Phenylacetamide-3-Chloromethylcephlenoic Acid p-Methoxybenzyl Ester (GCLE for short) is a pharmaceutical intermediate, especially used to synthesize cephalosporin antibiotics. At present, a small number of domestic manufacturers have produced it in small quantities. GCLE, but there are still problems in the production process, the production cost is high, and the product quality is poor. In its synthesis in China, penicillin potassium salt is mainly used as raw material, which is obtained through esterification, oxidation, ring expansion, reduction and chlorine gas, and the key final chlorine Chlorization reaction can be synthesized by chlorine gas method and tert-butyl hypochlorite method, but chlorine gas method is dangerous to use chlorine gas, and tert-butyl hypochlorite method is too costly to be suitable for industrialized production