Catalyst- and Solvent-Free Coupling of 2-MethylQuinazolinones and Isatins: An Environmentally Benign Access of DiastereoselectiveSchizocommunin Analogues

摘要

An environmentally benign highly atom-economic protocol for the construction of the C–C bond has been developed under catalyst- and solvent-free conditions. This protocol involves the efficient coupling of 2-methyl quinazolinones with isatin for the highly diastereoselective access of schizocommunin derivatives in excellent yields (up to 97%). Furthermore, the preliminary cytotoxicity screening of selected schizocommunin analogues displayed promising anticancer activity against human cancer cell lines, and the cytotoxic potential of active compound >12ac was also validated by in silico molecular docking simulation studies.