头孢地尼的绿色合成工艺

Green Synthesis of Cefdinir

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.