基本信息:
- 专利标题： 8-氯-1-环丙基-7-氟-9-甲基-4-氧-4-氢-喹嗪-3-羧酸酯及其合成方法
- 专利标题（英）：8-chloro-1-cyclopropyl-7-fluoro-9-methyl-4-oxo-4-hydroxy-quinolizine-3-carboxylate and synthetic method thereof
- 申请号：CN201610952553.6 申请日：2016-10-27
- 公开(公告)号：CN106543170A 公开(公告)日：2017-03-29
- 发明人： 马振坤 , 贺世杰 , 丁俊
- 申请人： 丹诺医药(苏州)有限公司
- 申请人地址： 江苏省苏州市苏州工业园区星湖街218号生物纳米园B2楼711室
- 专利权人： 丹诺医药(苏州)有限公司
- 当前专利权人： 丹诺医药(苏州)有限公司
- 当前专利权人地址： 江苏省苏州市苏州工业园区星湖街218号生物纳米园B2楼711室
- 代理机构： 江苏圣典律师事务所
- 代理人： 王玉国
- 主分类号： C07D455/02
- IPC分类号： C07D455/02
The invention provides 8-chloro-1-cyclopropyl-7-fluoro-9-methyl-4-oxo-4-hydroxy-quinolizine-3-carboxylate and a synthetic method thereof. The synthetic method comprises the following steps: a compound 6 and tert-butyldimethylsilyl chloride react in a first solvent under the effect of alkali to obtain a compound 12; the compound 12 and 3-ethoxy-2-fluoroacryloyl chloride react in a second solvent in a low-temperature condition under the effect of alkali to obtain a compound 13; the compound 13 and acid react in a third solvent to form a ring to obtain a compound 15; the compound 14 reacts in a chlorine hydride/methanol or chlorine hydride/ethanol liquid to obtain a compound 15; and the compound 15 and phosphorus oxychloride react in a fourth solvent to obtain the end product. The synthetic method provided by the invention carries out ring closing reaction first and hydrolysis of cyano groups second, and can effectively improve the yield of intermediate steps.
公开/授权文献:
- CN106543170B 8-氯-1-环丙基-7-氟-9-甲基-4-氧-4-氢-喹嗪-3-羧酸酯及其合成方法 公开/授权日：2018-02-23
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D455/00 | 杂环化合物，含有喹嗪环系，例如吐根碱生物碱，原小檗碱；二苯并 |
| --------C07D455/02 | .含有不进一步稠合的喹嗪环系 |