![3-羟甲基-7β-苯乙酰氨基-3-头孢-4-羧酸二苯甲酯的制备方法](/CN/2009/1/19/images/200910099186.jpg)
基本信息:
- 专利标题: 3-羟甲基-7β-苯乙酰氨基-3-头孢-4-羧酸二苯甲酯的制备方法
- 专利标题(英):Preparation method of 3-hydroxymethyl-7beta-phenylacetyl-3-cephalo-4-diphenylmethyl carboxylate
- 申请号:CN200910099186.X 申请日:2009-05-27
- 公开(公告)号:CN101570544A 公开(公告)日:2009-11-04
- 发明人: 孙楠 , 俞克平 , 胡信全 , 莫卫民 , 顾士崇
- 申请人: 浙江工业大学
- 申请人地址: 浙江省杭州市下城区朝晖六区
- 专利权人: 浙江工业大学
- 当前专利权人: 浙江工业大学
- 当前专利权人地址: 浙江省杭州市下城区朝晖六区
- 代理机构: 杭州天正专利事务所有限公司
- 代理人: 黄美娟; 冷红梅
- 主分类号: C07D501/30
- IPC分类号: C07D501/30 ; C07D501/06
The invention provides a preparation method of 3-hydroxymethyl-7beta-phenylacetyl-3-cephalo-4-diphenylmethyl carboxylate. The invention uses 7-ACA as starting material and uses the technical route of acetylation of first 7-amino phenylacetyling and then removal of 3-acetylation by hydrolysing via alkali to prepare intermediate 3-hydroxymethyl-7beta-3-cephalo-4-carboxylate, avoiding generation of 3-O-phenylacetyl side products without protecting process and deprotecting process. During the preparation process of 4-diphenylmethyl-acrylation of intermediate, the ethyl acetate solution of diphenylmethyldiazomethane is directly added into the mixed solution after the hydrolysis reaction and the hydrochloric acid is dripped to accelerate the esterification reaction, avoiding the generation of lactone of 3-hydroxymethyl-7beta-3-cephalo-4-carboxylate and promoting the generation of methyl-esterification of diphenyl. The target product is washed by reflowing in acetone and the purity thereof is greater than 99%. The invention has the advantages of simple operation, moderate reaction conditions, high yield, high purity of the product, etc.
公开/授权文献:
- CN101570544B 3-羟甲基-7β-苯乙酰氨基-3-头孢-4-羧酸二苯甲酯的制备方法 公开/授权日:2011-07-13
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D501/00 | 杂环化合物,含有5-硫杂-1-氮杂双环 |
--------C07D501/02 | .制备 |
----------C07D501/16 | ..在位置2和3之间有1个双键 |
------------C07D501/20 | ...7-酰基氨基头孢霉素酸或取代的7-酰基氨基头孢霉素酸,其酰基是由羧酸衍生的 |
--------------C07D501/24 | ....有被杂原子或杂环取代的烃基连在位置3 |
----------------C07D501/26 | .....被氧原子取代的亚甲基;及其带有2-羧基的内酯 |
------------------C07D501/30 | ......有被芳脂族羧酸酰化的7-氨基 |