Synthesis of 5,7-dihydrodibenzo[b,f][1,7]naphthyridine-6,12-dione, an unexpected isolate from Isatis tintoria

Herbert M. Riepl, Melanie Kellermann

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Abstract

The dye plant Isatis tinctoria yields a number of heterocyclic compounds with interesting anti-inflammatory and cytotoxic properties, formed mainly in an unknown manner by post-harvest treatment. A synthesis of the incidently isolated 5,7-dihydrodibenzo[b,f][1,7]naphthyridine-6,12-dione (4a) is presented. Starting from different 1,2-diarylhydrazines, adducts 11 with acetylenedicarboxylates (=but-2-ynedioates) are thermally treated (Scheme). In a Fischer-type rearrangement, 3-(arylamino)quinolinecarboxylic acids 9 are obtained, which can be cyclized under Friedel-Crafts conditions to yield a number of analoga 4 of the title compound.

Original languageEnglish
Pages (from-to)668-676
Number of pages9
JournalHelvetica Chimica Acta
Volume92
Issue number4
DOIs
StatePublished - Apr 2009

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