Title:
フルメタゾンおよびその17-カルボキシルアンドロステン類似体の調製
Document Type and Number:
Japanese Patent JP4095018
Kind Code:
B2
Abstract:
A process for the preparation of high purity flumethasone in high yield involves C3 protecting 9,11beta-epoxy-17alpha,21-dihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione,21-acetate, fluorinating at 6alpha, removing the C3 protecting group, fluorinating the 9,11-epoxy group. The resulting flumethasone 21-acetate is treated with the methanolic potassium hydroxide in the presence of an oxidation agent, causing a simultaneous hydrolyzation and degradative oxidation, resulting in the formation of 6alpha,9alpha-difluoro-11beta,17alpha-dihydroxy-16alpha-methyl-17beta-carboxy-androsta-1,4-diene-3-one in high yield. Flumethasone 21-acetate is alternatively hydrolyzed to yield flumethasone free alcohol.
Inventors:
Bill Lux, Ivan
Mendes, Zita
Mendes, Zita
Application Number:
JP2003503644A
Publication Date:
June 04, 2008
Filing Date:
June 11, 2002
Export Citation:
Assignee:
Hobion Limited
International Classes:
C07J3/00; C07J5/00; C07J71/00; C07J75/00
Domestic Patent References:
| JP6279485A | ||||
| JP54157554A | ||||
| JP64025793A | ||||
| JP2002155098A | ||||
| JP60190792A | ||||
| JP51048649A | ||||
| JP8092278A |
Foreign References:
| US3068253 | ||||
| WO2002008243A1 | ||||
| US3636010 |
Attorney, Agent or Firm:
Takehiko Suzue
Satoshi Kono
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto
Satoshi Kono
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto