| 发明名称 |
PROCESS FOR ALKYNYLATING 16-SUBSTITUTED-17-KETO STEROIDS |
| 摘要 |
A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17α-ethynyl-17β-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate. |
| 申请公布号 |
US2015005518(A1) |
申请公布日期 |
2015.01.01 |
| 申请号 |
US201214367886 |
申请日期 |
2012.12.19 |
| 申请人 |
CRYSTAL PHARMA, S.A.U. ;THE POPULATION COUNCIL INC. |
发明人 |
Gutiérrez Fuentes Luis Gerardo;Sandoval Rodríguez Celso Miguel |
| 分类号 |
C07J75/00;C07J31/00;C07J7/00;C07J51/00;C07J1/00 |
主分类号 |
C07J75/00 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
1. A process for the preparation of 16-methylene-17α-ethynyl-17β-hydroxy steroids, which comprises
(a) treating a 16-methylene-17-keto steroid with a compound of formula (I) wherein each R is independently selected from substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted aryl and halogen, and (b) desilylating the resulting 16-methylene-17α-silylethynyl-17β-hydroxy steroid. |
| 地址 |
Boecilillo-Valladolid ES |
