文摘
One-pot synthesis of tetracyclic naphthoxazole derivatives from electron-deficient naphthoquinones and alkynes was achieved via Rh(III)-catalyzed C鈥揌 activation and Csp3鈥揌 bond cleavage for the first time. This approach proceeds through a tandem cascade process involving substrate tautomerization, C鈥揌 activation, oxidative addition, cyclization, and aromatization. In addition, broad substrate scope, simple starting materials, and steric tolerance make this strategy of great practicality.