A review. Thiophene-2-carboxaldehyde was a kind of important pharmaceutical intermediate. Synthesis methods of thiophene-2-carboxaldehyde were reviewed from thiophene and N,N-dimethylformamide via condensation under phosphorus oxychloride, hydrolysis, neutralization and refined preparation The application of thiophene-2-carboxaldehyde in pharmaceutical synthetic aspect such as tenylidone, pyrantel, teniposide and 2-(2-thienyl)ethylamine was reviewed in detail. Also, some suggestions were put forward on production application and market development of thiophene-2-carboxaldehyde.