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First synthesis of 10 alpha-(trifluoromethyl)deoxoartemisinin
Fatima Chorki1, Fabienne Grellepois, Benoit Crousse
1BioCIS, Centre d'Etudes Pharmaceutiques, rue J.B. Clément, Châtenay-Malabry F-92296 Cedex, France.
Organic Letters
|March 1, 2002
Abstract:
[reaction: see text] A novel, nonacetal (trifluoromethyl)deoxoartemisinin was prepared with good stereoselectivity. This compound was obtained by debromination of the 10 alpha-CF3-10-bromodeoxoartemisinin in the presence of tributyltin hydride at reflux in toluene without alteration of the endoperoxide bridge. It presented a reasonable antimalarial activity.