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Parallel synthesis of 1,2,4-triazole derivatives using microwave and continuous-flow techniques

Abstract An efficient and convenient solution-phase synthesis of a 1H-1,2,4-triazole library with potential agrochemical activity is reported employing microwave-assisted organic synthesis (MAOS) and continuous-flow microfluidic synthetic methods starting from commercially available 3,5-dibromo-1H-1,2,4-triazole (1). MAOS was used for the synthesis of 5-amino-3-bromo-1,2,4-triazole analogs 3 and for their 3-aryl derivatives 4 via Suzuki–Miyaura coupling with polymer-supported catalyst. A microfluidic hydrogenation reactor integrated into an automated parallel synthesis platform was built and utilized for the reductive dehalogenation reactions providing 5-aminotriazoles (5). Graphical Abstract

Authors:   Tamás Szommer, András Lukács, József Kovács, Miklós J. Szabó, Michael G. Hoffmann, Monika H. Schmitt, János Gerencsér
Journal:   Molecular Diversity
Year:   2012
DOI:   10.1007/s11030-012-9357-2
Publication date:   25-Jan-2012
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