Pentacyclic triterpenes, especially ursolic and betulinic acid, are extracted eco-friendly from natural sources and are biologically active compounds. Semisynthesis tools have been employed in order to improve their biological activities. The bromination reaction could influence in the conformational structure of triterpenes skeleton and consequently, in their biological activity. In this work, we aim to survey and discuss an effective approach for semi-synthesis reactions to obtain betulinic acid (BA) and ursolic acid (UA) brominated derivatives and to evaluate their effects on viability of promastigote forms of Leishmania amazonensis. The bromination reaction protocol using N-bromosuccinimide (NBS) reagent was adapted for both triterpenes, aiming to obtain UA C12-Br and BA C30-Br modifications. The evaluation of leishmanicidal potential was performed using promastigotes forms of Leishmania (Leishmania) amazonensis and the viability was measured by MTT assay. According to spectroscopic data, the semi-synthesis of brominated triterpene derivatives using the methodology proposed was successfully accomplished. Bromination of the triterpene structures resulted in an increased antileishmanial activity comparing with the natural precursors, UA and BA. This report brings forth the discussion about the UA bromolactonization and BA C30-Br derivative semi-synthesis and characterization, and reports for the first time the activity of these derivatives on the viability of L. amazonensis, causative agent of leishmaniasis, a neglected tropical disease.