6,7,8,9-tetrahydro-2,12-dimethoxy-7-methyl-6-phenethyl-5H-dibenz[d,f]azonin-1-ol hydrochloride

Originator

Asocainol,ZYF Pharm

Manufacturing Process

A solution of a Grignard reagent is prepared from 5.5 g (0.23 mol) activated magnesium turnings and 41.5 g (0.24 mol) phenethyl bromide in 200 ml anhydrous diethyl ether. To this is added dropwise, at 35-40°C, a solution of 31.5 g (0.1 mol) thebaine in 0.4 liters dry benzene. After heating under reflux for 2 hours, the reaction mixture is decomposed with a solution of 48 g ammonium chloride in 200 ml water. The usual working up, after conversion of the base into the hydrochloride by means of hydrogen chloride in ethyl acetate, gives 7.3 g (21% of theory) (+/-)-2,12-dimethoxy-1-hydroxy-7- methyl-6-phenethyl-5,6,8,9-tetrahydro-7H-dibenz[d,f]azonine hydrochloride, melting point 227.6°C, after recrystallization from propan-2-ol.

Therapeutic Function

Antiarrhythmic

Raw materials

Preparation Products