Work

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

Year: 2025

Type: article

Abstract: 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.

Source: Asian Journal of Organic Chemistry

DOI: 10.1002/ajoc.202500634

Authors: Xuan Liu, Yujie Zou, Puying Luo, Yan Hong, Liu Yang, Qiuping Ding

Institutions: Jiangxi Normal University, Nanchang University, Jiangxi Maternal and Child Health Hospital

Language: English

Topic: Synthesis and pharmacology of benzodiazepine derivatives

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: bronze

Funders: National Natural Science Foundation of China, Natural Science Foundation of Jiangxi Province, Major Discipline Academic and Technical Leaders Training Program of Jiangxi Province