N-Heterocyclic Carbene-Catalyzed Formal [3+3] Annulation of Alkynyl Acylazoliums for the Synthesis of Benzofuro[3,2- b]pyridin-2-ones
Through β-activation of alkynoic acid esters with N-heterocyclic carbene catalysis, a formal [3+3] annulation of alkynyl acylazoliums with indolin-3-ones has been developed for the rapid construction of structurally interesting benzofuro[3,2-b]pyridin-2-ones with potential bioactivities. This protocol provides a highly efficient and simple method for the synthesis of the target molecules under mild reaction conditions with a wide substrate scope and excellent chemoselectivity. The synthetic utility of this protocol was also demonstrated by the versatile late-stage modifications.
2,4-Diaryl benzofuro[3,2-b]pyridine derivatives: Design, synthesis, and evaluation of topoisomerase inhibitory activity and cytotoxicity
Designed and synthesized twenty-four 2,4-diaryl benzofuro[3,2-b]pyridine derivatives were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Various aryl groups such as phenyl, 2-