Rutaecarpine belongs to the quinazolinocarboline type of alkaloids isolated from the fruits of Evodia rutaecarpa, which has been used in traditional Chinese medicine under the name Wu-Zhu-Yu against e.g. headache, dysentery, cholera, worm infections and postpartum disturbances. In literature, rutae-carpine and its derivatives have been reported to have cycloxygenase (COX-2) inhibitory, hypotensive, an-tiarrhythmic, antiplatelet aggregation, vasorelaxation and anti-anoxic activities. Owing to its pharmaceutical activities, attention is still focused on the development of new synthetic methods for rutaecarpine. Several methods of synthesis of rutaecarpine are reviewed according to the types of building chemical structures. Rutaecarpine was mostly made by tryptamine and anthranilic acid or their derivaties through complicated steps. So, the simple and convenient methods are still needed.

Key words: tryptamine, biosynthesis, anthranilic acid, synthesis, rutaecarpine