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.