GCLE3-位硫取代产物的合成及反应动力学研究  

Synthesis and Kinetics of 3-position Sulfur Substitution of GCLE

作　　者：范继业[1] 

机构地区：[1]河北化工医药职业技术学院制药工程系,河北石家庄050026

出　　处：《河北化工》2011年第11期25-26,29,共3页Hebei Chemical Industry

基　　金：河北化工医药职业技术学院资助项目(yz0808)

摘　　要：以7-苯乙酰氨基-3-氯甲基头孢烷烯酸对甲氧基苄酯(简称GCLE)取代7-ACA,直接和三嗪环反应合成头孢曲松中间体7-苯乙酰氨基-3-三嗪环甲基头孢-4-羧酸对甲氧苄酯,通过高效液相色谱仪对反应过程进行监测。研究了该反应的动力学,确定反应为SN2历程,通过测定25℃、35℃下在不同溶剂中反应的速率常数,得出其亲核取代反应活性顺序为:乙腈>四氢呋喃。7-Phenylacetamido-3-triazine-4-carboxylic acid p-methoxybenzyl ester was prepared by reaction of 7-phenglacetamido-3-chloromethyl-3-cephem-4-carboxylic acid p-methoxybenzyl estrer GCLE with triazine.The reaction process was inspected by HPLC.It was determined that the nucleophilic substitution reaction was 2nd order reaction.By determining the rate constants at 25 ℃ and 35 ℃ in different solvents,the activity order of the nucleophilicity was as follows： acetonitriletetrahydrofuran.

关 键 词：GCLE 7-苯乙酰氨基-3-三嗪环甲基头孢-4-羧酸对甲氧苄酯 合成 动力学 

分 类 号：R978.11[医药卫生—药品]