Betulinic acid (I) was extracted from the dried leaves of Syzygium claviforum. Acylation of (I) with 2,2-dimethylsuccinic anhydride (II) in the presence of DMAP in refluxing pyridine furnished the target 3?3?dimethylsuccinyl betulinic acid along with minor amounts of the undesired 2?2?dimethyl regioisomer (III), which were separated by means of preparative HPLC.