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Synthesis of 1,5-disubstituted-1H-tetrazole methane-linked bis-heterocycles via Ugi-azide

A series of twelve new 1,5-disubstituted-1H-tetrazoles were synthesized via Ugi-azide. The products were synthesized in moderate to excellent yields (50-96%). Methane-linked bis-heterocycles play a relevant role in medicinal chemistry. Tetrazole and furan heterocyclic moieties are present in many drugs. It has been well documented that both moieties could improve parameters of bioactive products such as bioavailability, lipophilicity and metabolic resistance.

Keywords: Ugi-azide, Tetrazoles, Furans, bis-heterocycles, MedChem.