A　novel　environment-friendly　method　to　access　bioactive　oroxin　A　through　a　one-pot/two-step　process　from　naturally　abundant　and　inexpensive　baicalin　is　described.　The　procedure　presented　here　has　several　advantages　including　clean,　one-pot,　synthetic　ease,　and　large-scale　feasibility.　This　work　also　provides　a　model　strategy　for　rapid　and　diverse　access　to　natural　molecules　sharing　the　common　skeleton　of　this　family.