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Short Paper | Regular issue | Vol 85, No. 3, 2012, pp.677-688
Published online, 17th February, 2012
DOI: 10.3987/COM-11-12414
Synthesis of Analogues of Makaluvamine A

Sébastien Bouclé and Jérôme Guillard*

*EA 3857 Laboratoire de Synthèse et Physicochimie, Organique et Thérapeutique, UFR des Sciences Pharmaceutiques, University of Tours, 31 Avenue de Monge, 37200 Tours, France

Abstract

A new and efficient synthesis of tricyclic pyridoquinonoxalinone 1 an analog of Makaluvamine A and its intermediates 2 and 3 has been developed starting from 5,8 dimethoxy-4,4 dimethyl[1,2,3,4]tetrahydroquinoline 4. The synthesis was accomplished in 11 steps and 4% overall yield from commercially available 2,5-dimethoxyaniline.