A Practical and Scalable Preparation of Lusianthridin

Abstract The efficient preparation of the stilbenoid lusianthridin is described. This synthesis relies on a Suzuki–Miyaura coupling and an intramolecular nucleophilic substitution as key reactions to construct the 9,10-dihydrophenanthrene core. The synthesis is completed in seven steps with a 13.2% overall yield, and each step can be conducted on a >20 gram scale. The route has provided 20 grams of lusianthridin for further biological activity studies.