![一种恩替卡韦的制备方法](/CN/2017/1/79/images/201710395764.jpg)
基本信息:
- 专利标题: 一种恩替卡韦的制备方法
- 申请号:CN201710395764.9 申请日:2017-05-31
- 公开(公告)号:CN107163049B 公开(公告)日:2019-06-18
- 发明人: 孙华君 , 杨尚金 , 朱毅 , 熊先胜 , 谢国范 , 赵涛涛 , 雷大有 , 何本斌 , 郭晨
- 申请人: 湖北远大生命科学与技术有限责任公司
- 申请人地址: 湖北省黄石市阳新县富池镇王坟路12号
- 专利权人: 湖北远大生命科学与技术有限责任公司
- 当前专利权人: 湖北远大生命科学与技术有限责任公司
- 当前专利权人地址: 湖北省黄石市阳新县富池镇王坟路12号
- 代理机构: 宜昌市慧宜专利商标代理事务所
- 代理人: 彭娅
- 主分类号: C07D473/18
- IPC分类号: C07D473/18 ; C07D307/935 ; C07B53/00
The invention relates to a preparation method of entecavir. The method comprises the steps: by adopting butanedial as a raw material, firstly synthesizing optically pure double-loop olefine aldehyde in the presence of a catalytic amount (R)-proline and dibenzylamine trifluoroacetate, protecting hydroxyl by using methyl, and carrying out decarbonylation by utilizing chlorotris(triphenylphosphine)-rhodium as a catalyst to obtain (3aS, 6aR)-2-methoxyl-3,3a-6,6a-tetrahydro-2H-cyclopentano [b] furan; carrying out Prins reaction in the presence of sulfuric acid to obtain a reduzate of Corey lactone, carrying out deprotection on all hydroxyls by using TBS, selectively removing a 2-bit protecting group and carrying out decarboxylic reaction in the presence of lead acetate to obtain a methylene compound; and finally introducing guanine by adopting a conventional method and carrying out deprotection to obtain the entecavir. By adopting butanedial as an initial raw material, the method has less than ten steps, and is mild in reaction condition, available in raw material and reagent, simple in operation, moderate in yield and suitable for industrial production.
公开/授权文献:
- CN107163049A 一种恩替卡韦的制备方法 公开/授权日:2017-09-15
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D473/00 | 含嘌呤环系的杂环化合物 |
--------C07D473/02 | .有氧、硫或氮原子直接连在位置2和6 |
----------C07D473/18 | ..1个氧原子和1个氮原子,例如鸟嘌呤 |