Quinazoline derivatives are part of many pharmaceutical drugs having medicinal applications such as sedatives, anti-malarial agents and in cancer treatment. Not many methods for their direct synthesis are available. A new solvent-free methodology using Ga(OTf)3 as a catalyst has been developed for the direct synthesis of difluoromethylated and trifluormethylated tetrahydroqiunazoline derivatives from the corresponding amines and fluorinated hemiacetals with high yields (40-94%). The green protocol is mild and efficient, useful for the preparation of many novel fluoromethylated tetrahydroquinazolines, which can be screened for potential therapeutic activites.

Direct synthesis of tetrahydroquinazolines

243rd National Meeting (2012)

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