Title:
PRODUCTION OF OLEANOLIC ACID DERIVATIVE
Document Type and Number:
Japanese Patent JP3453188
Kind Code:
B2
Abstract:
PURPOSE: To industrially and advantageously obtain an oleanolic acid useful as a production intermediate, etc., for endothelin receptor antagonism, etc., by reducing a specific steroidal lactone compound with an alkali(earth)metal in an amine solution.
CONSTITUTION: This oeanolic acid derivative is efficiently obtained by reducing a lactone compound expressed by formula I [either one of X and Y is H and the other is a (protected)hydroxy or X and Y together form aprotected)oxo; R2 is O, a (protected)hydroxyimino or a (protected)imino; R3 is an ester type hydroxy-protecting group] with an alkali metal (e.g. lithium) or an alkali earth metal in an amine solution under conditions of Birch reaction. The derivative is useful as a production raw material, etc., for various useful substances, e.g. endothelin receptor antagonism expressed by formula II (R1 is hydroxy or amino).
Inventors:
Miki Araki
Kazuhiro Takahashi
Isao Horibe
Toshiro Konoike
Kazuhiro Takahashi
Isao Horibe
Toshiro Konoike
Application Number:
JP10817894A
Publication Date:
October 06, 2003
Filing Date:
May 23, 1994
Export Citation:
Assignee:
Shionogi Pharmaceutical Co., Ltd.
International Classes:
C07J53/00; C07C51/09; C07C62/32; C07J63/00; C07J75/00; (IPC1-7): C07J63/00; C07J53/00; C07J75/00
Other References:
Ｔｅｔｒａｈｅｄｒｏｎ，Ｓｕｐｐｌｅｍｅｎｔ，（１９６６），Ｎｏ．７，ｐ．５７−６７
Attorney, Agent or Firm:
Aoyama Ryo (2 outside people)
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