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苄青霉素亚砜对-甲氧基苄酯的合成研究
引用本文:杨莉 徐满才 刘智凌. 苄青霉素亚砜对-甲氧基苄酯的合成研究[J]. 中国抗生素杂志, 2005, 30(10): 586-587,637
作者姓名:杨莉 徐满才 刘智凌
作者单位:[1]湖南师范大学化学化工学院,长沙410081 [2]湖南化工研究院,长沙410007
摘    要:以苄青霉素钾盐为原料,用低浓度CH3CO3H作氧化剂.所得苄青霉素亚砜以固体形式直接从溶液中结晶析出,再以对-甲氧基苄氯酯化,制得头孢类药物的母核7-苯乙酰胺基-3-氯甲基头孢烷酸对甲氧苄酯(GCLE)的关键中间体苄青霉素亚砜对-甲氧基苄酯,实验总收率82.6%。本工艺只使用一种有机溶剂,缩短了皮应时间,降低了成本,适合规模生产。

关 键 词:苄青霉素亚砜酯 头孢素菌 GCLE
文章编号:1001-8689(2005)10-0586-02
收稿时间:2005-03-08
修稿时间:2005-03-08

Synthesis of benzylpenicillin sulfoxide p-methoxybenzyl ester
Yang LI, Xu Man-cai, Liu Zhi-ling. Synthesis of benzylpenicillin sulfoxide p-methoxybenzyl ester[J]. Chinese Journal of Antibiotics, 2005, 30(10): 586-587,637
Authors:Yang LI   Xu Man-cai   Liu Zhi-ling
Affiliation:1 Department of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081 ; 2 Hunan Research Institute of Chemical Industry, Changsha 410007
Abstract:Benzylpenicillin potassium salt was oxidized by low concentration peracetic acid,the product could precipitate directly from the solution.Benzylpenicillin sulfoxide p-methoxybenzyl ester,the key intermediate for the preparation of the new nucleus,7-benzylacetamide-3-chloromethyl-3-cepham-4-carboxylic acid(p-methoxybenzyl) ester(GCLE) was synthesized by esterification with p-methoxybenzyl chloride.The overall yield was 82.6%.Only one organic solvent was needed to achieve the process in a reduced time and low cost and also could be used for scale-up production.
Keywords:Benzylpicillin sulfoxide ester    Cephalosporin   GCLE
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