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Title:
PRODUCTION OF PHENANTHRENE DERIVATIVE AND DIOXOPHENANTHRENE DERIVATIVE
Document Type and Number:
Japanese Patent JPH061746
Kind Code:
A
Abstract:

PURPOSE: To provide a new intermediate compound capable of stereoselectively synthesizing a high-purity dioxophenanthrene derivative useful as an IL-1 inhibitor in large quantity.

CONSTITUTION: The compound of formula I (R1 to R3 are lower alkyl) [e.g. 3,4,4a,9,10,10a-hexahydro-1-ethoxycarbonyl-1,4a-dimethyl-5,8-dimethoxy-7-(1- methylethyl)-2 (1H)-phenanthrenone], the compound of formula II and the compound of formula III (e.g. 5,8-dimethoxy-1,4a-dimethyl-7-isopropyl-3,4,4a,9,10,10a- hexahydro-2-phenanthrenecarboxylic acid). The compound of formula I and formula III can be produced from a compound of formula V derived from 4- bromo-2-isopropylphenol of formula IV and the compound of formula II can be produced by reducing the compound of formula I. Oxidation of the above compounds gives dioxophenanthrene derivatives of formula VI to formula VIII useful as IL-1 inhibitors.


Inventors:
Goto, Kiyoto
Shibuya, Masayuki
Shishido, Kozo
Application Number:
JP1993000013510
Publication Date:
January 11, 1994
Filing Date:
January 29, 1993
Export Citation:
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Assignee:
OTSUKA PHARMACEUT FACTORY INC
International Classes:
C07C67/343; C07C43/23; C07C46/00; C07C46/02; C07C50/34; C07C50/38; C07C66/00; C07C69/757; (IPC1-7): C07C50/34; C07C43/23; C07C46/00; C07C46/02; C07C50/38; C07C66/00; C07C67/343; C07C69/757
Attorney, Agent or Firm:
三枝 英二 (外4名)