摘要
以D-7-ACA为原料,经甲基化、 N-酰化和酯化反应等合成了头孢泊肟酯。对反应温度、 pH值、原料配比和催化剂等因素进行了工艺优化。通过IR、1H NMR、13C NMR和ESI-MS确证了头孢泊肟酯及中间体的结构。该工艺操作简单,原料价廉易得,总收率54.9%,产品纯度98.4%,具有工业化应用前景。
Cefpodoxime proxetil(1)was synthesized from D-7-ACA via the processes of methylation,N-acylation and esterification with a total yield of 54.9%and a purity of 98.4%.The affecting factors including the reaction temperature,pH value,the ratio of materials and the catalyst were investigated.The structures of the product and intermediates were characterized by IR,1 H NMR,13 C NMR and ESI-MS.The preparation process was simple in operation,low in raw material cost,and suitable for industrial production.
作者
陈经伟
靳文胜
陈涛
胡浩强
程青芳
CHEN Jing-wei;JIN Wen-sheng;CHEN Tao;HU Hao-qiang;CHENG Qing-fang(Zhejiang Kangle Pharmaceutical Co.,Ltd.,Wenzhou 325013,China;Jiangsu Key Lab of Marine Pharmaceutical Compound Screening,Lianyungang 222005,China)
出处
《精细化工中间体》
CAS
2019年第1期18-22,共5页
Fine Chemical Intermediates
基金
江苏省海洋药物活性分子筛选重点实验室开放基金(2015HYB02)
关键词
头孢泊肟酯
酯化
甲基化
N-酰化
cefpodoxime proxetil
esterification
methylation
N-acylation