Facile construction of pyrrolo[1,2-b]isoquinolin-10(5H)-ones via a redox-amination-aromatization-Friedel-Crafts acylation cascade reaction and discovery of novel topoisomerase inhibitors
Facile construction of pyrrolo[1,2-b]isoquinolin-10(5H)-ones via a redox-amination-aromatization-Friedel-Crafts acylation cascade reaction and discovery of novel topoisomerase inhibitors
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通过氧化还原-胺化-芳构化-Friedel-Crafts酰化级联反应轻松构建吡咯并[1,2-b]异喹啉-10(5H)-酮并发现新型拓扑异构酶抑制剂
DOI：
10.1039/c6cc03071h
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发表时间：
2016
影响因子：
4.9
通讯作者：
Wang Wei
中科院分区：
文献类型：
--
作者：
Wu Shanchao;Liu Na;Dong Guoqiang;Ma Lin;Wang Shengzheng;Shi Wencai;Fang Kun;Chen Shuqiang;Li Jian;Zhang Wannian;Sheng Chunquan;Wang Wei
以反式-4-羟基脯氨酸和2-甲酰基苯甲酸为原料，经氧化还原-胺化-芳构化-Friedel-Crafts酰化级联反应合成了吡咯并[1，2-B]异喹啉-10（5 H）-酮。化合物3 h被鉴定为一种新的有效的拓扑异构酶I/II双重抑制剂。
An efficient redox-amination–aromatization–Friedel–Crafts acylation cascade process from trans-4-hydroxyproline and 2-formylbenzoic acids has been developed for the synthesis of pyrrolo[1,2-b]isoquinolin-10(5H)-ones. Compound 3h was identified as a new potent dual topoisomerase I/II inhibitor.