去乙酰基-7-氨基头孢烷酸二苯甲酯的合成

Synthesis of Benzhydryl 7-Amino-3-(hydroxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

头孢卡品酯是第四代头孢类抗菌素的重要品种,人们已经对以去乙酰基-7-氨基头孢烷酸(D-7ACA)为起始原料合成头孢卡品酯的工作进行了大量研究,其中大部分都涉及到D-7ACA上羧基的保护,因此,对D-7ACA的羧基保护的研究是非常重要的.以二苯基重氮甲烷和D-7ACA为起始原料,采用超声波辅助的方法,以70%的收率合成了去乙酰基-7-氨基头孢烷酸二苯甲酯.

Cefcapene Pivoxil is important one of the fourth generational cephalosporin antibiotics.The synthesis of Cefcapene Pivoxil from D-7ACA has been intensively studied.Normally,it is involved to pro-tect the carboxyl group of D-7ACA.Thus,it is very important to study the protection of carboxyl group of D-7ACA.Benzhydryl 7-amino-3-（hydroxymethyl）-8-oxo-5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxy-late was obtained from D-7ACA with diphenyldiazo-methane as protection reagent,enhanced by ultrasonic wave,in 70% yield.