PURPOSE: To obtain a new benzanilide deriv. useful as a 5-HT10 antagonist in the prophylaxis and treatment of depression and other central nervous system disorders.
CONSTITUTION: The benzanilide deriv. is a compd. of formula I (R1 is halogen, H, 1-6C alkyl or 1-6C alkoxy; R2 is (substd.) phenyl; R3 is piperazin-1-yl or the like; R4 and R5 are each H, halogen, OH, 1-6C alkoxy or the like), e.g. 4'-[(2-methoxyethoxy)methyl]-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'- methyl-[1,1'-biphenyl]-4-carboxamide. The compd. of the formula I is obtd. by reacting an aniline of formula II with a halophenyl compd. of formula III (Y is halogen or -OSO2CF3) and carbon monoxide in the presence of a catalyst such as a Pd salt in a solvent such as acetonitrile at -10 to 150°C. The benzanilide deriv. is useful in the treatment of mood disorders, anxiety, anamnesis dysfunction and eating behavioral disorders and in the treatment of Parkinson disease, endocrine disorders, etc.
UIRIAMU REONAADO MITSUCHIERU
JIYON BURADOSHIYOO
JIYON WATOSUN KURISUROO
IAN BAKUSUTAA KIYANBERU
