(±)-Indolizidine 209D is one of the alkaloids isolated from the skin secretions of certain neotropical frogs and exhibit a range of pharmacological properties, including blocking neuromuscu-lar transmission. Therefore, the synthesis of indolizidine 209D and more complex derivatives, have been the subject of several publications. The preparation pathways of indolizidine 209D and its derivatives are the subject of this review. In this paper, some highly regio-and stereoselective func-tionalization process were reviewed through the synthesis of the optically active (±)-indolizidine 209D. © 2021 Bentham Science Publishers.