The direct chemical derivatization of natural plant extracts that would enable the straightforward synthesis of natural plant-like molecules seemed to be far from reality due primarily to the inherently complex chemical property of the extract. After model studies, the envisioned derivatization was realized under the rationally designed Bucherer-Bergs reaction conditions to afford unnatural hydantoin with tetrasubstituted carbon from the ethyl acetate extract of Curcuma zedoaria. The reaction proceeded with enough chemoselectivity to identify the desired product from the mixture by the reliable guidance of spectroscopic analyses. (C) 2016 Elsevier Ltd. All rights reserved.