基本信息:
- 专利标题： 2型糖尿病药物西他列汀制备新方法
- 专利标题（英）：Novel preparation method for anti-type-II-diabetes drug sitagliptin
- 申请号：CN201710358037.5 申请日：2017-05-19
- 公开(公告)号：CN107129501A 公开(公告)日：2017-09-05
- 发明人： 刘雄利 , 田民义 , 姚震 , 刘雄伟 , 张敏 , 周英 , 俸婷婷 , 余章彪
- 申请人： 贵州大学
- 申请人地址： 贵州省贵阳市花溪区贵州大学北校区科学技术处
- 专利权人： 贵州大学
- 当前专利权人： 贵州大学
- 当前专利权人地址： 贵州省贵阳市花溪区贵州大学北校区科学技术处
- 代理机构： 贵阳中新专利商标事务所
- 代理人： 李亮; 程新敏
- 主分类号： C07D487/04
- IPC分类号： C07D487/04 ; C07D263/44 ; C07C269/00 ; C07C269/06 ; C07C271/22 ; C07C227/18 ; C07C229/24 ; C07B53/00 ; A61P3/10
The invention discloses a novel preparation method for an anti-type-II-diabetes drug sitagliptin. According to the invention, trifluorobenzene with a cheaper price is used as a fluorization reagent and a starting raw material and a basic skeleton of sitagliptin is successfully synthesized through effective acylation of trifluorobenzene and L-aspartic acid; a synthesis route in the invention, from starting raw material and final product, is completely different from schemes disclosed in the prior art; the route is optimized, and easily-available natural L-aspartic acid is used as a chiral source for successful synthesis of an optically pure sitagliptin product; the problems of asymmetric catalysis and complex splitting in the prior art are overcome; the method also effectively overcomes the problem of low yield of the basic skeleton of sitagliptin synthesized via Friedel-Crafts acylation of trifluorobenzene and improves yield; the method is lower in cost, more convenient to operate and more suitable for industrial production; and compared with the prior art, the method is simpler in the synthesis route and better in operability.
公开/授权文献:
- CN107129501B 2型糖尿病药物西他列汀制备新方法 公开/授权日：2019-05-21
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D487/00 | 在稠环系中含有氮原子作为仅有的杂环原子的杂环化合物，不包含在C07D451/00至C07D477/00组中 |
| --------C07D487/02 | .在稠合系中含有两个杂环 |
| ----------C07D487/04 | ..邻位稠合系 |