Title:
6ALPHA-METHYLPREDNISOLONE 17,21-DIESTER
Document Type and Number:
Japanese Patent JPS58208299
Kind Code:
A
Abstract:
NEW MATERIAL:A compound of formula I (R is lower alkyl, aryl; R' is lower alkyl, alkenyl, aryl).
EXAMPLE: 6α-Methylprednisolone 17,21-dibutyrate.
USE: Anti-inflammatory steroid for external use.
PREPARATION: 6α-Methylprednislone of formula II and an alkyl ester of RC(OR")3 (R" is lower alkyl) are heated to effect reaction to give 6α-methylpredonisolone 17,21-cyclic orthoester. Then, the product is subjected to ring-opening reaction usually in the presence of a weak acid to prepare 6α-methylprednisolone 17-ester of formula IV. The product is subjected to acylation of the hydroxyl in the 21-position with an acid halide of R'COX (X is halogen) in the presence of a base such as pyridine to give the compound of formula I .
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Inventors:
KAMANO NORIAKI
SUGAI SABUROU
OKAZAKI TOKUJI
YOSHIDA SEIICHIROU
AKABOSHI MITSUYA
SUGAI SABUROU
OKAZAKI TOKUJI
YOSHIDA SEIICHIROU
AKABOSHI MITSUYA
Application Number:
JP9138982A
Publication Date:
December 03, 1983
Filing Date:
May 31, 1982
Export Citation:
Assignee:
OTA SEIYAKU KK
International Classes:
C07J5/00; A61K31/57; A61P29/00; (IPC1-7): A61K31/57; C07J5/00
Domestic Patent References:
| JPS5686119A | 1981-07-13 | |||
| JPS5874698A | 1983-05-06 |
Attorney, Agent or Firm:
Takao Minami
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