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  • Several important pharmaceutical intermediates
    Nov 08, 2018

    What are the important pharmaceutical intermediates? Medicine is a product that is closely related to modern people's lives. With the development of human society, the types of medicine, the production technology of medicine, and the effect of medicine are getting better and better, but the development of medicine is inseparable. The development of pharmaceutical intermediates can also be said that the development of medicine has driven the development of pharmaceutical intermediates. The following is a brief introduction to several of the most important pharmaceutical intermediates:


    First, p-hydroxy-glycine

    Hydroxy-glycine is a medicinal fine chemical with a white crystalline powder. It is a side chain of synthetic β-lactams and semi-synthetic antibiotics. It is used in amoxicillin (commonly known as amoxicillin) cefoperazone, cefradine. Antibiotics such as pyridine, cefotaxime, ceftriaxone sodium and hydroxyl EPCP, 7ADCA, etc. These drugs are widely used, both injectable and orally. They are broad-spectrum antibacterial and anti-inflammatory drugs, which are obtained in the clinical treatment of gastric and duodenal ulcers. Satisfactory efficacy. It is an important pharmaceutical intermediate. In recent years, domestic demand is increasing year by year. It is expected that the demand will increase by 8% in the next five years, and the development prospect is broad.


    Second, α-methylene cyclic ketone

    Alpha-methylene cyclic ketone is an active center of many anticancer active drugs, and its α,β-unsaturated ketone structure belongs to a concealed group of anticancer active groups, and is important for the synthesis of many important cyclic anticancer drugs. Pharmaceutical intermediates.


    Third, 4,4'-dimethoxyacetoacetate methyl ester

    Methyl 4,4'-dimethoxyacetoacetate is an important intermediate for niphalpine, a therapeutic drug for cardiovascular and cerebrovascular diseases. Nilvadipine was developed by Fujisawa Pharmaceutical Co., Ltd., and the second-generation calcium antagonist was launched in 1989. The agent is currently the leading drug for cardiovascular and cerebrovascular diseases in the international market, and there is no domestic production. Methyl dimethoxyacetate is synthesized from glyoxylic acid as raw material and trimethyl orthoformate in the presence of concentrated sulfuric acid. The latter is reacted with methyl acetate and sodium methoxide to obtain 4,4'-dimethoxyacetoacetate. ester.


    Fourth, C3-chlorocephem

    C3-chlorocephemic acid is an important cephalosporin cefaclor intermediate. Cefaclor is a second-generation high-efficiency oral cephalosporin developed by American Lai Lai Company. Due to its obvious curative effect and oral superiority, it was in the United States in 2001. Sales reached more than 80 million yuan, ranking second in antibiotics. There are two kinds of C3-chlorocephemate synthesis routes. 1) The penicillin G salt is synthesized by oxidation, esterification, ring expansion, reduction, oxidation, reduction, oxidation, deacetylation, hydrolysis, etc., and there are too many steps. The yield is low; 2) 7-aminocephalosporanic acid (7-ACA) is used as raw material, and 7-ACA is highly active in the 7-position amino group and 4-position carboxyl group when the 3-position is modified. First, protection is required. 4-carboxyl protection is commonly used to prepare tert-butyl ester, diphenylmethyl ester and p-nitrobenzyl ester; 7-amino group can be protected by phenoxymethyl, benzyl, and trimethyl. Protected by a silylating agent such as chlorosilane.