Cascade Alkylation/Cyclization of ortho ‐Isocyanodiaryl Amines to Alkylated Dibenzodiazepines and Their Primary Activities

ABSTRACT A cascade alkylation/cyclization reaction of ortho ‐isocyanodiaryl amines with 1,3‐dicarbonyl compounds in the presence of Mn(OAc) 3 ·2H 2 O has been developed. This reaction offers an efficient protocol to alkylated dibenzodiazepines, and features simple and mild conditions, wide substrate scope, and good functional group tolerance. All of those examined products exhibited obvious cytotoxic activities against Hela, HepG‐2, SGC‐7901, and HL‐60 cells at 20 µM. Compounds 3f , 3i , and 3r show better activity than 5‐FU on SGC‐7901 cells.