A new and efficient multicomponent solid-phase synthesis of 2-acylaminomethylthiazoles |
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| Authors: | Bernd HenkelMichael Sax Alexander Dömling |
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| Institution: | a Morphochem AG, Gmunder Straße 37-37a, D-81379 München, Germany
b Westfälische Wilhelms-Universität Münster, Institut für Medizinische und Pharmazeutische Chemie, Hittorfstraße 58-62, D-48149 Münster, Germany |
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| Abstract: | A new multicomponent reaction (MCR) for the preparation of 2-substituted thiazole libraries using Rink amide resin is described. Thiazoles are assembled in a one-pot MCR of a thiocarboxylic acid, aldehyde, 3-(N,N-dimethylamino)-2-isocyanoacrylate with a resin-bound primary amine. Aliphatic and aromatic thiocarboxylic acids as well as aliphatic and (hetero-) aromatic aldehydes work in the reaction. Cleavage of the product yields the substituted thiazoles in reasonable to good purity. |
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