Title:Light Fluorous-Tagged Traceless One-Pot Synthesis of Benzimidazoles Facilitated by Microwave Irradiation
Volume: 15
Issue: 5
Author(s): Chih-Chung Tseng, Cheng-Hsun Tasi and Chung-Ming Sun
Affiliation:
Keywords:
Benzimidazoles, bioactive heterocycles, fluorous synthesis, F-SPE, microwave chemistry
Abstract: 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.