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Sequential Ugi/Heck cyclization strategies for the facile construction of highly functionalized N-heterocyclic scaffolds
Authors:Vijaya Gracias  Joel D. Moore  Stevan W. Djuric
Affiliation:Scaffold-Oriented Synthesis, Abbott Laboratories, Medicinal Chemistry Technologies, R4CP, AP10, 100 Abbott Park Road, Abbott Park, IL 60064-6099, USA
Abstract:A new strategy employing an Ugi four-component reaction and a microwave-assisted intramolecular Heck cyclization in a sequential fashion to access an array of N-containing heterocycles is reported. The two-step sequence generated compounds of significant molecular complexity from trivial starting materials in an expedient fashion with excellent yields. The route was also amenable to solid-phase chemistry demonstrating potential for library generation.
Keywords:Ugi   Heck   multi-component reaction   solid-phase   scaffold
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