以吡唑并[1,5-a]吡啶-2-甲醛和N-甲酰基哌嗪为原料,经过还原胺化反应、水解反应、N-烷基化反应,合成了2-[4-(4-氟苄基)哌嗪-1-基甲基]吡唑并[1,5-a]吡啶,总收率29.5%,用1HNMR、19FNMR、ESI-MS对中间体及目标化合物进行了结构表征,并通过体外受体结合实验,测定目标化合物对多巴胺D4受体的亲和常数为1.2nmol/L,对D2、D3受体的亲和常数分别为3 900、1 890 nmol/L,显示对多巴胺D4受体具有较高的亲和性与选择性,是一种潜在的多巴胺D4受体配基。 Pyrazolo [1,5-a] pyridine-2-carbaldehyde and N-formylpiperazine were synthesized by the reductive amination, hydrolysis and N-alkylation reactions to synthesize 2- [4- Fluorobenzyl) piperazin-1-ylmethyl] pyrazolo [1,5-a] pyridine was obtained in a total yield of 29.5%. The intermediate and the target compound were subjected to 1HNMR, 19F NMR and ESI- The affinity constants of the target compound to dopamine D4 receptor were determined to be 1.2 nmol / L and the affinity constants to D2 and D3 receptors were 3900 and 1890 nmol / L, respectively, by an in vitro receptor binding assay. It has a high affinity and selectivity for dopamine D4 receptor and is a potential dopamine D4 receptor ligand.