7, 8-OXIDE DERIVATIVE OF MORPHINAN

Title:

7, 8-OXIDE DERIVATIVE OF MORPHINAN

Document Type and Number:

Japanese Patent JPS572288

Kind Code:

A

Abstract:

NEW MATERIAL:The titled compounds of formula I (R1 is H, acyl; R2 is H; R3 is hydroxyl, acyloxy, or R2 and R3 incoporate to form oxo).

EXAMPLE: 3,6-Diacetylmorphine-7,8-oxide (Heroin-7,8-oxide).

USE: Durg having analgesic, antitussive and sedative activities. They have the same level of analgesic activity as morphine or heroin, being a metabolite of codeine.

PREPARATION: 3-Methoxymethylmorphinone of formula II is oxidized to give 3- methoxymethylmorphinone-7,8-oxide, which is reduced to form 3-methoxymethylmorphine-7,8-oxide. Then, the product is hydrolyzed to give morphine-7,8-oxide of formula Ia. Further the compound of formula Ia is acylated to produce 3,6-diacylmorphine-7,8-oxide of formula Ib (Ac is acyl).

Inventors:

MIYATA NAOKI
WATANABE KEIZOU
HIROBE MASAAKI

Application Number:

JP7474880A

Publication Date:

January 07, 1982

Filing Date:

June 03, 1980

Export Citation:

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Assignee:

KOWA CO
HIROBE MASAAKI

International Classes:

C07D491/18; A61K31/485; A61P11/14; A61P25/04; A61P25/20; C07D489/02; (IPC1-7): A61K31/485; C07D491/18

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