Nipecotic acid and its derivatives, which have high bioactivity, are significant pharmaceutical intermediates. In this review, the synthetic methods of nipecotic acid and its derivatives are summarized. The application of nipecotic acid and its derivatives to synthesizing drugs for γ-aminobutyric acid (GABA) uptake inhibition, cancer chemotherapy, growth hormone secretion, anti-inflammation, cardiovascular disease Alzheimer’s disease, nootropics, anti-flu virus and bone disease is presented as well.

Key words: nipecotic acid derivative, pharmaceutical intermediate, nipecotic acid