| Abstract
| - Thiazolo ring-fused 2-pyridones have proven to be highly interesting scaffolds for the development ofbiologically active compounds. Many methods are today available to introduce a variety of substituentsin the 2-pyridone part of the heterocycle. Herein we disclose how a diverse set of substituents can beintroduced in the thiazolo ring, with possibilities to vary also the spatial arrangement of the substituents.A key intermediate is the oxidized framework 9 for which an effective synthesis is described. The thiazolopart of this system can be substituted either via conjugate additions, resulting in trans selectivity, or viamicrowave-assisted Heck couplings that result in unsaturated aryl-substituted analogues. The scaffoldcan also be lithiated followed by the addition of various electrophiles, which increases the diversificationpotential substantially, as exemplified with the introduction of halogens, alkyl, acyl, and amide substituents.
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