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Trifluoromethyl substituted quinolines are the subject of growing interest because of their medicinal importance, particularly as antimalarial agents (e.g., mefloquine and halofantrine). 3 Since the classical antimalarial molecules are encountering increased drug resistance, considerable efforts have been directed toward the synthesis of new fluorinated quinolines that can provide improved anti-parasitic activity. 4 The purpose of this work is to report the results of a chemical behavior study of the reactions of ketones 1 with 2,6-diaminotoluene (2,6-DAT).

Highly Efficient Synthesis of CF3-Containing 7-Aminoquinolines From Cyclocondensation Reaction of Trifluoroacetyl Enamine Precursors