Microwave-assisted Cu-catalyzed C-C bond formation: one-pot synthesis of fully substituted 1,2,3-triazoles using nonsymmetrical iodoalkynes and their biological evaluation

摘要

A copper-catalyzed one-pot synthesis of fused benzothiazino[1,2,3] triazolo[4,5-c]quinolinone derivatives from 1-iodoalkynes with different aryl azides via an in situ generated 5-iodotriazole intermediate in [BMIM]PF6 under microwave irradiation is reported. The reaction provided the desired fused 1,2,3-triazoles in good to excellent yields. Anticancer activity of the synthesized compounds has been screened in vitro against different cancer cell lines (MCF-7, HeLa, A-549, and IMR-32). Some of the derivatives showed remarkable anticancer activity against two cancer cell lines - MCF-7 and A-549. The remaining compounds have shown good to moderate activity against tested cell lines.