2-[4-(4-Fluorobenzyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine was synthesized from pyrazolo[1,5-a]pyridine-2-carbaldehyde and 1-piperazinearboxaldehyde through reductive amination, amide hydrosis and N-alkylation. The structures of the intermediates and the target compound were confirmed by 1H NMR, 19F NMR and ESI- MS. Through in vitro receptor binding assay, the affinity constants of the target compound were determined to be 1.2, 3900 and 1890 nM for D4, D2, D3 receptor, respectively. It indicated that 2-[4-(4-fluorobenzyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine is a potential dopamine D4 receptor ligand.