The reaction of 4,4,4-trifluoro-3-oxobutanoates with the corresponding electron-rich amino heterocycles was investigated. A simple and flexible general procedure for the regiospecific annulation of the trifluoromethylpyridine ring to electron-rich amino heterocycles was proposed. A set of CF 3 -containing fused pyridines in almost quantitative yield was obtained.

Fused pyridine derivativesFused pyridine derivatives R 0450 Electron-Rich Amino Heterocycles for Regiospecific Synthesis of Trifluoromethyl-Containing Fused Pyridines. -The reaction of a variety of electron-rich amino heterocycles with trifluoromethyl-containing 1,3-diones is studied. A general reaction is found to yield CF3-substituted fused pyridines. 4,4,4-Trifluoro-3-oxobutanoate (XIII) gives a hydroxy-substituted fused pyridine (XIV) under similar conditions. The OH-group allows further derivatization. -(VOLOCHNYUK*, D. M.; PUSHECHNIKOV, A. O.; KROTKO, D. G.; SIBGATULIN, D. A.; KOVALYOVA, S. A.; TOLMACHEV, A. A.; Synthesis 2003, 10, 1531-1540; Res. Dev. Cent. Chem. Biol., Taras Shevchenko Univ., Kiev 252033, Ukraine; Eng.) -Mais 47-142

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