
基本信息:
- 专利标题: 5-(4-溴苯基)-4,6-二氯嘧啶的制备方法
- 专利标题(英):Preparation method of 5-(4-bromophenyl)-4,6-dichloropyrimidine
- 申请号:CN201810905221.1 申请日:2018-08-09
- 公开(公告)号:CN108997223A 公开(公告)日:2018-12-14
- 发明人: 高飞飞 , 高军龙 , 朱敏亮 , 卢娓 , 柳毅
- 申请人: 浙江先锋科技股份有限公司
- 申请人地址: 浙江省台州市临海市涌泉后泾岩头
- 专利权人: 浙江先锋科技股份有限公司
- 当前专利权人: 浙江先锋科技股份有限公司
- 当前专利权人地址: 浙江省台州市临海市涌泉后泾岩头
- 代理机构: 北京科家知识产权代理事务所
- 代理人: 张安心
- 主分类号: C07D239/30
- IPC分类号: C07D239/30
The invention belongs to the technical field of pharmaceutical chemistry synthesis, and relates to a preparation method of 5-(4-bromophenyl)-4,6-dichloropyrimidine. The preparation method comprises the following steps: carrying out catalytic esterification on bromophenylacetic acid to prepare methyl p-bromophenylacetate, then carrying out a reaction with dimethyl carbonate to synthesize 2-(4-bromophenyl)-malonic acid-1,3-diethyl ester, carrying out cyclization by using formamidine hydrochloride to obtain 5-(4-bromophenyl)-4,6-dihydroxy pyrimidine, and then carrying out chlorination to obtain the product 5-(4-bromophenyl)-4,6-dichloropyrimidine. In the preparation process of the intermediate 1, a solid acid is adopted as a catalyst, so that the synthesis process and a post-treatment step are simplified. The solid acid is easy to separate and can be repeatedly used, so that resources are saved, and production cost is reduced. In a process of preparing the intermediate 2, sodium methoxideis adopted as an alkali to replace sodium hydride or amino sodium used in the prior art, so that production safety is improved, and production cost is reduced. Meanwhile, the intermediate 3 is prepared by adopting a one-pot method, so that operation steps are reduced.
公开/授权文献:
- CN108997223B 5-(4-溴苯基)-4,6-二氯嘧啶的制备方法 公开/授权日:2020-06-30
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D239/00 | 杂环化合物,含1,3-二嗪环或氢化1,3-二嗪环 |
--------C07D239/02 | .不与其他环稠合 |
----------C07D239/06 | ..环原子间或环原子与非环原子间有1个双键 |
------------C07D239/28 | ...有杂原子或有以3个键连杂原子、其中最多以1个键连卤素的碳原子,直接连在环碳原子上 |
--------------C07D239/30 | ....卤素原子或硝基 |