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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. | LitMetric
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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.

Shanchao Wu Na Liu Guoqiang Dong Lin Ma Shengzheng Wang Wencai Shi Kun Fang Shuqiang Chen Jian Li Wannian Zhang Chunquan Sheng Wei Wang

Chem Commun (Camb)

School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China and Department of Chemistry and Chemical Biology, University of New Mexico, Albuquerque, NM87131-0001, USA.

Published: July 2016

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.

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 Source
http://dx.doi.org/10.1039/c6cc03071hDOI Listing

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