Title:
The manufacturing process of an esthetic trawl
Document Type and Number:
Japanese Patent JP6254289
Kind Code:
B2
Abstract:
The invention relates to a process for obtaining Estetrol or a salt or solvate thereof, the process comprising: a) reacting a compound of formula (IV) or a salt or solvate thereof, wherein R1 is a hydroxyl protecting group selected from a silyl ether, an ether, an ester, a carbamate and a carbonate, and R2 is a hydroxyl protecting group selected from an ether, with an oxidizing agent selected from OsO4 or a source of osmium tetroxide to produce Estetrol or a compound of formula (II) or a salt or solvate thereof wherein R1 is as defined previously; and b) if a compound of formula (II) is obtained in step a), deprotecting said compound to produce Estetrol.
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Inventors:
Juan, Jose, Ferreira, Hill
Jesus, Miguel, Iglesias, Retuelt
Francisco, Javier, Gajo, Nieto
Jesus, Miguel, Iglesias, Retuelt
Francisco, Javier, Gajo, Nieto
Application Number:
JP2016543386A
Publication Date:
December 27, 2017
Filing Date:
September 17, 2014
Export Citation:
Assignee:
CRYSTAL PHARMA,S.A.U.
International Classes:
C07J1/00
Foreign References:
| WO2013012328A1 | ||||
| WO2013034780A1 | ||||
| WO2013050553A1 |
Other References:
SUZUKI, Emako, et al.,Steroids,1995年,60,277-284
NAMBARA, Toshio, et al.,Steroids,1976年,27(1),111-122
KAMIKUBO, Takashi, et al.,Chemistry Letters,1996年,11,987-988
SEREBRENNIKOVA, G. A., et al.,Journal of Organic Chemistry of the USSR,1967年,3,2048-2050
NAMBARA, Toshio, et al.,Steroids,1976年,27(1),111-122
KAMIKUBO, Takashi, et al.,Chemistry Letters,1996年,11,987-988
SEREBRENNIKOVA, G. A., et al.,Journal of Organic Chemistry of the USSR,1967年,3,2048-2050
Attorney, Agent or Firm:
Hiroyuki Nagai
Yukitaka Nakamura
Yasukazu Sato
Satoru Asakura
Mari Asano
Hiroshi Sorimachi
Yuko Matsuyama
Yukitaka Nakamura
Yasukazu Sato
Satoru Asakura
Mari Asano
Hiroshi Sorimachi
Yuko Matsuyama