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Synthesis of 14-Azacamptothecin, a Water-Soluble Topoisomerase I Poison

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journal contribution
posted on 03.03.2005, 00:00 by Nicolas J. Rahier, Kejun Cheng, Rong Gao, Brian M. Eisenhauer, Sidney M. Hecht
14-Azacamptothecin, a potent, water-soluble analogue of the antitumor agent camptothecin, has been prepared by a convergent synthesis. The key condensation of the AB and DE rings with concomitant formation of ring C of 14-aza CPT was carried out in two stages, the latter of which involved a radical cyclization strategy.