METHOD FOR PREPARING DERIVATIVES OF MORPHINONE, METHOD FOR PREPARING DERIVATIVES OF 14-HYDROXYMORPHINONE AND METHOD FOR PREPARING DERIVATIVE OF OXYMORPHONE Russian patent published in 2004 - IPC

FIELD: organic chemistry, chemical technology, medicine, narcology.

SUBSTANCE: invention relates to a method for preparing derivatives of morphinone that are intermediate compounds used for preparing derivatives of 14-hydroxymorphinone that, in turn, are used for preparing antagonists of opiates - derivatives of oxymorphone. Method for preparing derivatives of morphinone involves oxidation of derivatives of morphine of the general formula (I):

with hypochlorous and hypobromous acid salts wherein in indicated formula (I) R means lower alkyl, (C₃-C₆)-cycloalkyl, benzyl or substituted benzyl, cyano-group; R₁ means alkyl, benzyl or alkylcarbonyl; R₂ means hydrogen atom, alkyl, benzyl or alkylcarbonyl. Oxidation is carried out with hypochlorous and hypobromous acid salts prepared preferably before oxidation immediately. For oxidation sodium and potassium hypochlorites or hypobromites are used preferably. Antagonists of opiates are important medicinal agents used for treatment and diagnosis of narcomania.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

7 cl, 3 ex