4-[2-(2-氨基-4,7-二氢-4-氧-1H-吡咯[2,3-d]嘧啶-5-基)乙基]苯甲酸的中试生产  

Industrial producing of 4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolopyrimidin-5-yl)ethyl]benzoic

作　　者：祝莉霞[1] 彭苏[1] 赵一农[1] 

机构地区：[1]南京制药厂有限公司,南京210038

出　　处：《药学与临床研究》2009年第3期210-211,共2页Pharmaceutical and Clinical Research

摘　　要：目的:研究培美曲塞二钠的关键中间体4-[2-(2-氨基-4,7-二氢-4-氧-1H-吡咯[2,3-d]嘧啶-5-基)乙基]苯甲酸的放大生产。方法:以对碘苯甲酸甲酯为起始原料,经缩合、溴代、环合、水解等反应得到制备培美曲塞二钠的关键中间体。结果:总收率约36.8%,本方法操作简单,收率稳定,适合工业化生产。Objective： To synthesize the intermediates of pemetrexed disodium. Methods： 4- [ 2- （2-amino-4,7-dihydro-4-oxo-1 H-pyrrolo [ 2,3-d] pyrimidin-5-yl ） ethyl] benzoic acid was prepared via condensation, bromination, cyclization, hydrolysis reaction and so on. Result： The overall yield was about 36.8%. This process is suitable for industrial producing and easy to operate, and their yield is stable.

关 键 词：4-[2-(2-氨基4 7-二氢-4-氧-1H-吡咯[2 3-d]嘧啶-5-基)乙基]苯甲酸 中间体 培美曲塞二钠 抗 肿瘤药物 

分 类 号：R914.5[医药卫生—药物化学]