Method for making tetrabenazine compounds

摘要: A method of preparing a tetrabenazine compound (TBZ compound) having structure I comprising the steps reacting nucleophilic alkenyl species with aldehyde II and oxidizing resultant allylic alcohol to provide enone III. The protecting group P1 on tetrahydroisoquinoline nitrogen is removed deprotected intermediate induced undergo an amino cyclization reaction product TBZ I. may be used prepare either enantiomeric form tetrabenazine; (+)-tetrabenazine or (-)-tetrabenazine. Alternatively adapted mixture enriched in one enantiomer, racemic mixture, diastereomeric compounds. In addition, present invention provides novel synthetic compositions which both enantiomers tetrabenazine, derivatives analogs tetrabenazine.