7-氨基-3-乙烯基 头孢烷酸的一步法环保制备方法  

One-step environment friendly preparation method of 7-amino-3-vinyl cephalosporanic acid

作　　者：徐鑫林 梁丙辰 姜鹏鹏 Xu Xinlin;Liang Bingchen;Jiang Pengpeng(Hebei Hejia Pharmaceutical Technology Group Corporation Ltd.,Shijiazhuang 052165,China;Hebei Hejia Pharmaceutical Science and Technology Group,Hejia Research Institute,Shijiazhuang 050035,China)

机构地区：[1]河北合佳医药科技集团股份有限公司,河北石家庄052165 [2]河北合佳医药科技集团合佳研究院,河北石家庄050035

出　　处：《煤炭与化工》2021年第5期125-128,共4页Coal and Chemical Industry

摘　　要：7-氨基-3-乙烯基-4-头孢烷酸(7-AVCA)是头孢克肟和头孢地尼的药用中间体。为解决7-AVCA合成过程中收率低、环境污染严重等难题,通过改造D-7-ACA的分子结构,提出了一种全新的制备7-AVCA的一步法环保合成工艺。D-7-ACA经P.C.C氧化后,与甲基三苯基溴翁盐进行Wittig反应,制备得到7-AVCA。实验结果表明,该合成工艺较原有工艺操作简单、原子利用率高,所制备的7-AVCA产品物质的量收率约为62.0%,纯度约为99.1%。7-Amino-3-vinyl-4-cephalosporanic acid(7-AVCA)is a pharmaceutical intermediate of cefixime and cefdinir.In order to solve the problems of low yield and serious environmental pollution in the synthesis process of 7-AVCA,a new one-step environment friendly synthesis process for the preparation of 7-AVCA was proposed by modifying the molecular structure of D-7-ACA.7-AVCA was prepared by Wittig reaction of D-7-ACA oxidized by P.C.C with methyl triphenyl bromide salt.The experimental results show that the synthesis process was simpler and higher atomic utilization rate than the original process,and the molar yield of the prepared 7-AVCA product was about 62.0%,and the purity was about 99.1%.

关 键 词：D-7-ACA 7-AVCA 甲基三苯基溴翁盐 WITTIG反应 绿色合成工艺 

分 类 号：TQ463.5[化学工程—制药化工]