Synthesis of Naphthalene Natural Products Dehydrocacalohastine and Musizin

Abstract Natural methylated naphthalene compounds, possessing diverse biological activities, remain to be studied because of low content in plants and lacking synthetic methods. Herein, we have disclosed new approaches to methylated naphthalene natural products represented by dehydrocacalohastine and musizin from simple and commercially available naphthalene molecules with the assistance of our reported regioselective C−H methylation. The dehydrocacalohastine has been firstly synthesized from 1‐bromonaphthalen‐2‐ol in overall 8.9% yield with 8 steps. Additionally, the solution to musizin saved 2 steps with comparative yields to previous reported route.