| 发明名称 | Process and intermediates for the preparation of abiraterone acetate | ||
| 摘要 | The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes. | ||
| 申请公布号 | US8975244(B2) | 申请公布日期 | 2015.03.10 |
| 申请号 | US201414176463 | 申请日期 | 2014.02.10 |
| 申请人 | Mapi Pharma Ltd. | 发明人 | Marom Ehud;Rubnov Shai;Mizhiritskii Michael |
| 分类号 | C07D211/68;A61K31/58;C07J43/00 | 主分类号 | C07D211/68 |
| 代理机构 | Rothwell, Figg, Ernst & Manbeck, P.C. | 代理人 | Rothwell, Figg, Ernst & Manbeck, P.C. |
| 主权项 | 1. A process for the preparation of (3β)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate represented by the structure of formula (1), and salts thereof the process comprising the steps of: a) coupling a protected dehydroepiandrosterone (10) with a pyridinyl derivative (11) to form a pyridinyl hydroxy derivative (12): wherein PG is a hydroxyl protecting group; andM is selected from the group consisting of Li, Na, K, MgX, ZnX, CdX, Si(R)3, Ge(R)3 and Sn(R3); wherein X is a halogen and R is a substituted or unsubstituted alkyl, cycloalkyl, alkylaryl or aryl; b) converting compound (12) to (17-pyridin-3-yl)-androsta-5,16-diene (13):and c) transforming compound (13) into (3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-ol (Abiraterone acetate) (1). | ||
| 地址 | Ness Ziona IL | ||