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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Light Fluorous-Tagged Traceless One-Pot Synthesis of Benzimidazoles Facilitated by Microwave Irradiation

Author(s): Chih-Chung Tseng, Cheng-Hsun Tasi and Chung-Ming Sun

Volume 15, Issue 5, 2012

Page: [411 - 417] Pages: 7

DOI: 10.2174/138620712800194521

Price: $65

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.

Keywords: Benzimidazoles, bioactive heterocycles, fluorous synthesis, F-SPE, microwave chemistry


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