基本信息:
- 专利标题： 一种达泊西汀及其中间体的合成方法
- 专利标题（英）：Synthetic method of dapoxetine and intermediate thereof
- 申请号：CN201911193728.X 申请日：2019-11-28
- 公开(公告)号：CN110845369A 公开(公告)日：2020-02-28
- 发明人： 许丹倩 , 夏爱宝 , 白亮 , 盘龚健
- 申请人： 浙江工业大学
- 申请人地址： 浙江省杭州市下城区潮王路18号
- 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潮王路18号
- 代理机构： 杭州天正专利事务所有限公司
- 代理人： 黄美娟; 俞慧
- 主分类号： C07C269/06
- IPC分类号： C07C269/06 ; C07C271/12 ; C07C271/18 ; C07C271/16 ; C07C315/00 ; C07C317/28 ; C07C213/08 ; C07C215/28 ; C07C213/06 ; C07C217/48
The invention discloses a synthetic method of dapoxetine and its intermediate, i.e., (S)-3-(tert-butyloxycarbonyl)amino-3-phenylpropanol as shown in a formula 5 which is described in the specification. The synthetic method of (S)-3-(tert-butyloxycarbonyl)amino-3-phenylpropanol is as shown in a synthesis route which is described in the specification, wherein a compound 3 and acetaldehyde are subjected to a Mannich reaction in an organic solvent under the action of a supramolecular catalyst constructed by a chiral catalyst and a polymer so as to obtain a compound 4, and the polymer is at least one selected from of the group consisting of PEG 200, PEG 400, PEG 600, MeOPEG 750, PEG 800, PEG 1000, PPG 800 and PPG 1000. The dapoxetine is synthesized from the (S)-3-(tert-butyloxycarbonyl)amino-3-phenylpropanol prepared by using the above method according to steps as shown in the synthesis route. The synthetic method of dapoxetine and the intermediate thereof has the characteristics of usage of cheap and easily available raw materials, high yield and low cost, and is more beneficial to industrial production.
公开/授权文献:
- CN110845369B 一种达泊西汀及其中间体的合成方法 公开/授权日：2022-03-18
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07C | 无环或碳环化合物 |
| ------C07C269/00 | 氨基甲酸的衍生物，即含有如下任何基团的化合物NCOO，NCOHal，NCOO，NCOHal或NCHalHal，氮原子不属于硝基或亚硝基的制备 |
| --------C07C269/06 | .由不涉及形成氨基甲酸酯基的反应 |