| 摘要 |
PURPOSE: To obtain a new compound having dopamine-2 receptor antagonistic action and serotonin-2 receptor antagonistic action, and useful as a therapeutic or improving agent for cerebrovascular lesions, the aggressive behavior, psychostimulation, fugue, delire, clairsentience and hyperkinesis each involved in senile dementia, schizophrenia, depression, etc. CONSTITUTION: This compound is expressed by formula I (R<1> is H, a halogen, a lower alkyl, etc.; R<2> and R<3> are each H, a halogen, a lower alkyl, etc.; R<4> is H, a halogen, a lower alkyl, etc.;R<5> is H, a lower alkyl, a heteroarylalkyl, etc.; (n) is 0-3), e.g. 1-[3-(2-cyanophenyl)-4-chloro-5-(1- fluoropropyl)]phenylpiperazine. The compound of formula I is obtained by the following process: a phenylpiperazine derivative of formula II is first protected and then reacted with an alkylmagnesium halide, and the product is reacted with a halogenating agent followed by reaction with 2-(1,3,2-dioxabornan-2-yl) benzaldehyde, etc., in the presence of tetrakis(triphenylphosphine)palladium(0) and cesium carbonate. |
