A novel protocol for rapid assemble of benzimidazole framework has been demonstrated. This method
incorporated with light fluorous-tag provides a convenient method for diversification of benzimidazoles and for easy
purification via fluorous solid-phase extraction (F-SPE) in a parallel manner. The key transformation of this study
involves in situ reduction of aromatic nitro compound, amide formation, cyclization and aromatization promoted by
microwave irradiation in a one-pot fashion. The strategy is envisaged to be applied for the establishment of drug-like
small molecule libraries for high throughput screening.
Keywords: Benzimidazoles, bioactive heterocycles, fluorous synthesis, F-SPE, microwave chemistry
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