头孢地尼的绿色合成工艺  

Green Synthesis of Cefdinir

作　　者：汤有坚 徐辉 丁志亮 钟为慧[2] 

机构地区：[1]浙江永宁药业股份有限公司,台州318020 [2]浙江工业大学药学院,杭州310014

出　　处：《浙江化工》2013年第4期8-10,共3页Zhejiang Chemical Industry

基　　金：浙江省重大科技专项(2009C01029-3)

摘　　要：用乙酰基替代三苯甲基保护去甲氨噻肟酸乙酯中的肟羟基,使头孢地尼活性酯与7-AVCA的缩合反应和肟羟基的去保护反应合二为一;用绿色溶剂2-甲基四氢呋喃替代二氯甲烷,应用于头孢地尼的合成;将副产物三苯基氧膦和2-巯基并噻唑回收并再生为三苯基膦和DM,循环利用,从源头上减少了三废排放量,具有工业化应用前景。Using triphenylmethyl instead of acetyl to protect hydroxyl group in ethyl 2-（2- aminothiazole-4-yl）-2-hydroxyiminoacetate, so the condensation of Cefdinir active ester with 7-amino-3- vinyl-3-eephem-4-earboxylie acid （7-AVCA） and the deproteetion of hydroxyl group could be preceded successively. Green solvent 2-methyhetrahydrofuran （2-MeTHF） instead of diehloromethane was used for the preparation of Cefdinir. The reeyelization and reuse of the side product triphenylphosphine oxide and 2- mereaptobenzothiazole were investigated. The present method can reduce dramatically the amount of wastes, so it can be considered of good prospect for industrial application.

关 键 词：头孢地尼 2-甲基四氢呋喃 活性酯 绿色合成 

分 类 号：TQ463[化学工程—制药化工]