A naturally occurring enynyl-benzenoid, Benzocamphorin H (1), from the edible fungus Taiwanofungus camphoratus (Antrodia camphorata) was characterized by the comprehensive spectral analysis. It displayed potent anti-inflammatory bioactivity and would be valuable for further biological studies. The present study is the first total synthesis of Benzocamphorin H and the developed strategy described a more efficient procedure that allowed large-scale production of Benzocamphorin H for the further research of biological activity both in vitro and in vivo. (C) 2012 Elsevier Ltd. All rights reserved.