Visible‐light‐induced Difunctionalization of Styrenes with 4‐cyanopyridines and Thioacetates or Thiosulfonates

Abstract Simultaneous thiolation/pyridinylation of alkenes was achieved in a three‐component reaction under visible‐light‐induced conditions. By employing 4CzIPN as a photocatalyst and DIPEA as a base, a variety of alkenes and cyanopyridines reacted well with thioacetates or thiosulfonates to obtain the difunctionalized products in excellent yields with high regio‐selectivity. The thiolation/pyridinylation products could easily transfer to 4‐(1‐phenylvinyl)pyridine or dithioperoxoate compounds. Furthermore, the in vitro antitumor activities of selected compounds were screened through MTT assay and the results showed that compound 6 e exhibited similar antitumor activity with 5‐fluorouracil (5‐FU).