Efficient library synthesis of imidazoles using a multicomponent reaction and microwave irradiation

E. Gelens, F.J.J. De Kanter, R.F. Schmitz, L.A. Sliedregt, B.J. Van Steen, C.G. Kruse, R. Leurs, M.B. Groen, R.V.A. Orru

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

Optimization of Radziszewski's four-component reaction employing a microwave-assisted protocol, led to a small library of 48 imidazoles with a success rate of 65% (conversion >45%). All three diversity points of the four-component reaction were varied. Aromatic and aliphatic inputs were successfully implemented and mono-, di-, tri- and tetrasubstituted imidazoles with various substitution patterns were synthesized. Furthermore, unsymmetrical diketones could successfully be used which improved the intrinsic diversity of the method significantly. If the unsymmetrical diketone 1,2-phenylpropanedione (R
Original languageEnglish
Pages (from-to)17-22
JournalMolecular Diversity
Volume10
Issue number1
DOIs
Publication statusPublished - 2006

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