Abstract The first total synthesis of the novel anticancer agent kwanzoquinone C (1), an anthraquinone glycoside which has been isolated from extracts of the roots of orange daylilies (Kaempfer)(Hemerocallisfulva) is reported. The strategy involves the preparation of the tetrasubstituted 1, 3-butadiene 6 by an electrocyclic conrotatory ring opening of the cyclobutanone rac-11, which is obtained by a [2+ 2] cycloaddition. Diels–Alder reaction of ...