苯胺促进的异苯并呋喃酮类衍生物的合成  

Aniline-Promoted Synthesis of Isobenzofuranone Derivatives

作　　者：袁硕 王四喜 陈锦杰 赵龙飞 余斌[1,2,3,4] 刘宏民 Yuan Shuo;Wang Sixia;Chen Jinjie;Zhao Longfei;Yu Bin;Liu Hongmin(School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001;Co-Innovation Center of Henan Province for New Drug R &D and Preclinical Safety,Zhengzhou 450001;Key Laboratory of Technology of Drug Preparation,Ministry of Education,Zhengzhou 450001;Guangdong Provincial Key Laboratory of New Drug Screening,Guangzhou 510033)

机构地区：[1]郑州大学药学院,郑州450001 [2]新药创制与药物安全性评价河南省协同创新中心,郑州450001 [3]教育部药物关键制备技术重点实验室,郑州450001 [4]广东省新药筛选重点实验室,广州510033

出　　处：《有机化学》2018年第11期3009-3015,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.81430085;81773562;81703326);国家重点研发计划(No.2016YFA0501800);河南省科技攻关项目(No.182102310123);中国博士后面上基金(No.2018M630840);广东省新药筛选重点实验室开放课题(No.GDKLNDS-2018OF006);河南省高等学校重点科研项目(No.18B350009);郑州大学大学生创新创业训练计划(No.201810459101)资助项目~~

摘　　要：异苯并呋喃酮类化合物广泛存在于自然界中,并具有广泛的生物活性.报道了以邻羧基苯甲醛和不同取代的苯乙酮为原料,苯胺促进的串联反应构建异苯并呋喃酮类骨架结构的合成新方法,该方法具有适用范围广、反应条件温和、高产率和简单易处理等优点,为异苯并呋喃酮类化合物的合成提供了新思路.Isobenzofuranone derivatives are widely found in nature and have shown diverse biological activities.In this work,the aniline-promoted synthesis of isobenzofuranone derivatives starting from 2-carboxybenzaldehyde and substituted acetophenones under mild reaction conditions is reported.This method has broad substrate scope,high yields,and is operationally convenient,and therefore could serve as an attractive strategy for practical synthesis of isobenzofuranone derivatives.

关 键 词：异苯并呋喃酮 苯胺 串联反应 

分 类 号：O626[理学—有机化学]