METHOD OF PRODUCING HIGHLY PURE 4a,5,9,10,11,12-HEXAHYDRO-6H-BENZOFURO[3a,3,2-EN][2]BENZAZEPINE, AS WELL AS DERIVATIVES THEREOF Russian patent published in 2012 - IPC C07D491/06 A61K31/4355 A61K31/55 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing highly pure 4a,5,9,10,11,12-hexahydro-6H-benzofuro[3a,3,2-en][2]benzazepine, as well as derivatives thereof of formula I and II , produced from racemic bromonarwedine which is debrominated during catalysis with palladium. The invention involves treatment of the reaction mixture, which takes place in the presence of oxygen or peroxides, such that the palladium catalyst is converted to an insoluble, easily separated form. The following reactions take place via reduction of enantiomerically pure narwedine to enantiomerically pure galantamine, which is then alkylated or dealkylated so as to achieve the corresponding substitution in the nitrogen ring atom. Through subsequent purification such as recrystallisation, residual content of palladium lower than 5 ppm is achieved, which enables direct use as pharmaceutical raw material.

EFFECT: improved method.

6 cl, 4 tbl