To obtain a compound having excellent antiemetic activity based on its potent serotonin S3(5HT3) and dopamine D2 antagonistic action, thus useful for treating and preventing various digestive organ symptoms involved in various diseases and therapeutic methods.
This compound, a cyclic amine derivative, is expressed by formula I {X is CH or N; Y is (CH2)n, O, etc.; (n) is 1, 2 or 3; R1 is an alkyl, R2 is an alkoxyl; R3 is amino, a monoalkylamino, etc.; R4 is a halogen; wavy line means the steric configuration of the bound carbon atoms represents RS, R or S}, e.g. 5-chloro-N-(1-ethyl-1H-hexahydroazepin-3-yl)-2-methoxy-4- methylaminobenzamide. The compound of formula I is obtained by reaction of a compound of formula II with a compound of formula II in a solvent such as benzene pref. at about -10 to 150°C.
MORIE TOSHIYA
YAMAZAKI HIROSHI
YOSHIDA NAOYUKI
