TBHP-Mediated Oxidative Decarboxylative Cyclization in Water:Directand Sustainable Access to Anti-malarial Polycyclic Fused Quinazolinonesand Rutaecarpine  

作　　者：Xingyu Chen Fei Xia Yifan Zhao Ji Ma Yue Ma Dong Zhang Lan Yang Peng Sun 

机构地区：[1]Artemisinin Research Center and Institute of Chinese Materia Medica,Academy of Chinese Medical Sciences,Beijing 100700,China

出　　处：《Chinese Journal of Chemistry》2020年第11期1239-1244,共6页中国化学（英文版）

基　　金：Generaus financial support was from the National NaturalScience Foundation of China(Nos.21702235,81841001);the Fundamental Research Funds for the Central Public Welfare Research Institutes(Nos.ZZ13-YQ-098,ZZ10-024,ZXKT17053);the Major National Science and Technology Program of China forlnnovative Drug(No.2017ZX09101002-001-001).

摘　　要：of main observation and conclusion Polycylic fused quinazolinones with anti-malarial activity were synthesized through tert-butyl hydro-peroxide(TBHP)-mediated oxidative decarboxylative cyclization between commercaly vailable isatins and cylic amines in one step.The reaction pro-ceeds smoothly in water without additional ransition-metal catalyt,acid and base.The newly synthesied products were evaluated to exhibit moderateto good anti-malaril activity against chloroquine drug-sensitive Plasmodium falciparum 3D7 strain.Additionally this method aso provides direct approach to Rutaecarpine in good yield.

关 键 词：strain. smoothly OXIDATIVE 

分 类 号：O62[理学—有机化学]