Abstract The versatile preparation of permethylated anigopreissin A (1) has been accomplished from methyl 3, 5-dihydroxybenzoate. The key steps of the synthesis are sequential Sonogashira and Suzuki cross-couplings for the construction of the 2, 3- diarylbenzo [b] furan moiety and Wittig olefination for the introduction of the styryl group.