NEW DISUBSTITUTED TRANS-3,4,4A,5,6,10B-HEXAHYDRO-2H-NAPHTHO(1,2-B)-1,4-OXAZINE, ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

摘要

PROBLEM TO BE SOLVED: To produce a new compound capable of acting as a selective ligand on a specific dopaminergic receptor subtype and reducing adverse effects and useful for treating anxiety, depression, aggression, Parkinson disease and shizophrenia. SOLUTION: This compound in a racemic form or an optical isomeric form is represented by formula I (A is a 1-10C alkyl or the like; E is CN or the like) and its salt to which a pharmaceutically acceptable acid is added, e.g. trans-3,4,4a,5,6,10b-hexahydro-9-cyano-4-propyl-2H-naphtho[1,2-b]-1,4- oxazine. The compound represented by formula I is obtained by a method for reacting a trans compound represented by formula II with trifluoromethanesulfonic acid anhydride in the presence of pyridine and then reacting the resultant compound with zinc cyanide and Pd[P(C6 H5 )3 ]4 in dimethylformamide under heating or the like. The new compound is capable of selectively acting on D3 receptors.