Selective synthesis of fluorinated benzyl- or phenylpyrimidines from the heterocyclisation of alpha-trifluoroacetylarylpropanenitriles
Fiche publication
Date publication
septembre 2007
Auteurs
Membres identifiés du Cancéropôle Est :
Dr BERBER Hatice
Tous les auteurs :
Berber H, Mirand C, Derouin F
Lien Pubmed
Résumé
Some 5-benzyl-6-trifluoromethyl-2,4-diaminopyrimidines analogous to trimethoprim and 6-aryl -5-trifluoroethyl-2,4-diaminopyrimidines analogous to pyrimethamine were prepared from the same synthons, trifluoromethylated P-ketonitriles. The heterocyclisation between enol ether of beta-ketonitrile and guanidine leading to these compounds was studied. These fluorinated novel compounds were tested for their in vitro activity against Toxoplasma gondii, a widespread apicomplexan protozoa responsible for congenital toxoplasmosis and cerebral toxoplasmosis in immunocompromised patients. (c) 2007 Elsevier B.V. All rights reserved.
Référence
J Fluor Chem. 2007 Sep;128(9):1039-45