| 摘要 |
<p>Preparation of aryl piperazine compounds (I) comprises reacting aromatic halide compound (II) with piperazine in the presence of palladium complexes (which bear bisaryldialkylphosphine (III) as ligands) and alkali metal base. Preparation of aryl piperazine compounds of formula (I) comprises reacting aromatic halide compounds of formula (II) with piperazine in the presence of palladium complexes (which bear bisaryldialkylphosphine of formula (III) as ligands) and alkali metal base. Ar : mono-, bi- or tricyclic aromatic radical having a total of 5-18 ring atoms (where no or one ring atom per cycle is O, S, N) (optionally mono- or polysubstituted); Hal : Cl, Br or I; R 1>, R 2>1-12C alkyl or 5-11C arylalkyl; R 3>,R 4>H, 1-6C alkyl, 1-6C alkoxy or di-1-6C alkylamino; R 5>1-12C (fluoro)alkyl, 1-12C (fluoro)alkoxy, F, 4-10C aryl or 5-11C arylalkyl; and m, n : 0-3. [Image].</p> |
