| 发明名称 |
Methods for the synthesis of tiotropium bromide |
| 摘要 |
The present invention relates to methods for synthesizing tiotropium bromide following the scheme:;
Using the above scheme, tiotropium bromide (compound 6C) is obtained under mild conditions and with high yields. |
| 申请公布号 |
US9242979(B2) |
申请公布日期 |
2016.01.26 |
| 申请号 |
US201514605618 |
申请日期 |
2015.01.26 |
| 申请人 |
|
发明人 |
Bilgic Mahmut |
| 分类号 |
C07D491/08;A61K31/44;C07D451/00;C07D333/24;C07D491/18 |
主分类号 |
C07D491/08 |
| 代理机构 |
Clark & Elbing LLP |
代理人 |
Clark & Elbing LLP |
| 主权项 |
1. A synthesis method for preparation of tiotropium bromide, said method comprising:
a) transforming compound 1C (di-(2-thienyl) acetic acid)under conditions suitable for anhydride formation to obtain compound 2C (di-(2-thienyl)-acetic acid anhydride); b) reacting compound 2C with scopine to obtain compound 4C; c) converting compound 4C to compound 5C under conditions that do not require a purification procedure; and; d) oxidizing compound 5C to produce compound 6C |
| 地址 |
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