头孢他啶侧链活性硫酯合成的研究

Research on the Synthesis of Side Chain of Ceftazidime Activated Thioester

综述了以乙酰乙酸乙酯 ,乙酰羰基甲酸乙酯等原料合成头孢他啶侧链活性硫酯的方法 ,并建议开发以乙酰乙酸乙酯为起始原料 ,经溴化、肟化、成环 3步反应一锅合成中间体 2 -氨基 -α -羟亚氨基 - 4 -噻唑乙酸乙酯 ,继而经醚化、水解、酰化一锅合成目的产物的生产工艺。

In this paper, methods of synthesis of side chain of ceftazidime activated thioester are summarized.It was suggested to develop such a method to synthsesize the target product which used ethyl acetoacetate as raw material,carried out bromination, oximation and cyclocondensation in one pot to get the intermediate 2-amino-α-hydroxyimino-4-thiozoleacetic acid and then obtained the final product through etherify,hydrolysis and acylation in one pot.