Expedient Synthesis of Epigoitrin From L-Ascorbic Acid

Epigoitrin is the main bioactive constituent of an important traditional Chinese herbal medicine, Radix isatidis. Reported pharmacological effects of epigoitrin include antiviral, anticancer, and antithyroid activities. Extensive biological exploration of epigoitrin was constrained by the limited natural source. This article describes our continued effort toward chemical preparation of epigoitrin from the readily available L-ascorbic acid. Our new developed synthetic route is composed of nine steps, with an overall yield of 17%.