PURPOSE: To obtain a new 2-methoxyphenylpiperazine deriv. having pharmacological activity to the level of a serotonin 5-HTIA receptor.
CONSTITUTION: This 2-methoxyphenyl piperazine deriv. is a compd. represented by formula I [where A is CO, (CH2)nHNCO or (CH2)nHNCH2; (n) is 2-4 and B is a halogen, methoxymethyl, an (amino substd.) aryl, a heteroaryl, etc.] or its pharmacologically allowable acid added salt, e.g. N-[2-[4-(2- methoxyphenyl)piperazin-1-yl]ethyl]-4-amino-5-chloro-2-methoxybenzamide. The compd. represented by formula I is obtd. by bringing an amine, a compd. represented by formula II (where X is a halogen or an alkylamino having a carbon chain of 2-4 C atoms), benzoyl chloride substd. by one or more halogen, amino or methoxy groups or a hetero-arom. acid chloride having O, S or N as a hetero atom forming a part of a 5- or 6-membered ring, cyclo- or bicycloalkane, etc., into reaction at room temp. in an org. solvent in the presence of a basic medium to which an org. salt has been added.
RUISA ARONSO SHIRESU