TBHP-Mediated Oxidative Decarboxylative Cyclization in Water:Direct and Sustainable Access to Anti-malarial Polycyclic Fused Quinazolinones and Rutaecarpine

• 作者: Xingyu Chen Fei Xia Yifan Zhao Ji Ma Yue Ma Dong Zhang Lan Yang Peng Sun
• 来源期刊: 中国化学（英文版）
• 年，卷（期）: 2020,（11）
• 所属期刊栏目: Concise Reports
• 页码范围: 1239-1244
• 页数: 6页
• 语种: 英文
• DOI: 10.1002/cjoc.202000154

摘要

Polycyclic fused quinazolinones with anti-malarial activity were synthesized through tert-butyl hydro-peroxide(TBHP)-mediated oxidative decarboxylative cyclization between commercially available isatins and cyclic amines in one step.The reaction pro-ceeds smoothly in water without additional transition-metal catalyst,acid and base.The newly synthesized products were evaluated to exhibit moderate to good anti-malarial activity against chloroquine drug-sensitive Plasmodium falciparum 3D7 strain.Additionally,this method also provides direct ap-proach to Rutaecarpine in good yield.