NOVEL ARYLPIPERAZINYLALKYL-3(2H)-PYRIDAZINONE

摘要

PURPOSE: Provided is a novel compound, arylpiperazimylalkyl-3(2H)-pyridazinone, having high affinity to serotonin 5HT1A receptor and 5HT2 receptor, and dopamine D2 receptor, and useful as a nonspecific antipsychotic agent due to the presence of a 3(2H)-pyridazinone group. CONSTITUTION: The novel compound is arylpiperazimylalkyl-3(2H)-pyridazinone represented by the formula(I), wherein R1 is methyl or phenyl; R2 is H or methyl; n is 2-4; R3 is a (substituted) naphthyl or phenyl|, e.g. 6-methyl-2-(4-(4-naphthylpiperazin-1-yl)butyl)-3(2H)-pyridazinone. It is manufactured by condensing a compound of formula(II) in which Z is Cl or Br with a piperazine of formula(III) in the presence of a base at a temperature within the range from 20 deg.C to the boiling point of the reaction mixture in an inert solvent. The compound of formula(II) can be obtained by reacting an alkyl dihalide with a compound of formula(IV) in a nonprotonic solvent or in dimethylformamide with solid potassium hydroxide at a temperature within the range from room temperature to 100 deg.C in the presence of a strong base.