PURPOSE: To obtain a new compound having a strong antagonistic effect on serotonin S2 receptor, therefore, effective for negative symptoms of schizophrenia and useful as an antipsychotic agent reduced in extrapyramidal side effects and a therapeutic agent for anxiety syndrome, depression, etc.
CONSTITUTION: A compound of formula I [R1 is H, a lower alkyl, phenyl, etc.; R2 and R3 are eachH, a halogen, a lower alkyl, etc.; R4 is H or a lower alkyl; (m) is 2 or 3; (n) is 3 or 7] and its salt, e.g. 2-(4-flurophenyl)-4-94-methyl-1- piperazinyl)-6,7,8,9-tetrahydro-5H-cycloheptapyrimidine. This compound is synthesized by reacting a compound of formula II (X is an eliminable atom or an eliminable group) with a compound of formula III generally at 40 to 200°C under ordinary pressure or applied pressure. In addition, the raw material compound of formula II is obtained, e.g. by using a compound of formula IV (Y is Cl or Br) as the starting raw material.
HINO KATSUHIKO
OCHI YOSHIAKI
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