文献类型：期刊文献

中文题名：头孢卡品酯合成工艺的化学原理解析

英文题名：Analysis of the Synthetic Process of Cefcapene Pivoxil by Principles of Chemistry

作者：冀亚飞[1];刘宏伟[1];赵建宏[1];管海英[2];廖道华[1];宋恭华[1]

机构：[1]华东理工大学药学院,上海200237;[2]上海新亚药业有限公司技术中心,上海201203

年份：2016

卷号：33

期号：4

起止页码：77

中文期刊名：化工高等教育

外文期刊名：Higher Education in Chemical Engineering

收录：国家哲学社会科学学术期刊数据库

基金：2015年度上海市教委本科重点课程建设项目(YC0126108);国家自然科学基金(21476074)项目

语种：中文

中文关键词：制药工艺学;案例教学;头孢卡品酯;反应原理;合成工艺

外文关键词：Pharmaceutical technology; Case teaching; Cefcapene pivoxil; Reaction principle; Synthetic technique

摘要：本文对新一代头孢菌素类药物头孢卡品酯的合成工艺进行了详细的化学原理解析,在每一操作步骤的过程化学解析基础上,给出了相应反应的科学工艺配置,以实现高效合成、连续反应、去除杂质、规避副反应、结晶分离纯化等操作目的。这些讨论涉及关键中间体Boc-Ⅲ-二异丙胺盐的合成和它的后续酯化反应,以及Boc-Ⅱ脱保护、成盐反应,以期获得目标产物头孢卡品酯单水合单盐酸盐。这个典型的原料药合成工艺案例被应用于教学。
The synthetic process of cefcapene pivoxil,a new generation of cephalosporin drugs,have been resolved in detail by principles of chemistry.Based on the interpretation of process chemistry for every operating step,the corresponding optimum processing techniques are allocated in order to achieve efficient syntheses,attain continuous reactions,circumvent side-reaction,realize crystallization,separation and purification of the products,and so on.These discussions involve the synthesis of Boc-Ⅲ-diisopropylammonium salt and its subsequent esterification,as well as the deprotection of Boc-Ⅱand sequential salification,finally obtaining the target product cefcapene pivoxil monohydrochloride monohydrate（Ⅰ）.The classical case of bulk pharmaceutical chemical has been applied in classroom teaching.