Betulin 1 is pentacyclic triterpenoid natural product that is obtained as secondary metabolite in more than 200 different types of plants. Betulin and its derivatives exhibit several important pharmacological properties such as antitumor, anti-inflammatory, antiparasitic, and anti-viral activities [1]. However, deeper studies showed that medicinal application of the majority of betulin derived molecules have been hindered by their poor water solubility. A possible option to overcome the low bioacessability of lipophilic triterpene core is introduction of polar functional groups [2]. The aim of this work is to obtain novel amino group bearing betulin derivatives by CH amination at C(16) of betulin core.