First synthesis of 10 alpha-(trifluoromethyl)deoxoartemisinin |
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| Authors: | Chorki Fatima Grellepois Fabienne Crousse Benoit Hoang Vu Dinh Hung Nguyen Van Bonnet-Delpon Danièle Bégué Jean-Pierre |
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| Institution: | BioCIS, Centre d'Etudes Pharmaceutiques, rue J.B. Clément, Chatenay-Malabry F-92296 Cedex, France. |
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| 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. |
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