[Show abstract][Hide abstract] ABSTRACT: This presentation will discuss approaches to enhance the rate of molecular probe discovery and close the growing knowledge
gap between chemical and biological space created by recent advances in systems biology. As such, multi-component reactions
are advocated as tools to build proprietary compound collections, founded on the central tenets of efficiency in medicinal
chemistry: (1) the potential for increased “iterative speed” around the “hypothesis–synthesis–screening” loop and (2) reduced
numbers of required iterations for expedited value chain progression. Front-loading collections, in this respect, have afforded
several successful “bench-to-bedside” studies with no required intermediate “scaffold hopping.” Such examples may be viewed
as the original “holy grail” of combinatorial chemistry, now enabled by the exponentially increasing MCR-derived “chemical
diversity space” made accessible in recent years.
Full-text · Article · Jan 2011 · Advances in Experimental Medicine and Biology
[Show abstract][Hide abstract] ABSTRACT: We present a convenient synthesis of novel pyrrole- and indole-fused 1-oxo-1,2,3,4-tetrahydropyrazine heterocyclic structures using a novel modification of four-component Ugi condensation. We demonstrate the usefulness and versatility of the developed approach for the synthesis of variously substituted compounds, and discuss the scope and limitations of the chemistry involved.Graphical abstract
No preview · Article · Jan 2005 · Tetrahedron Letters
[Show abstract][Hide abstract] ABSTRACT: We present a convenient synthesis of novel 3-oxo-1,2,3,4- tetrahydropyrrolo[1,2-a]pyrazine-1-carboxamides using a modification of four-component Ugi condensation. According to this method, (2-formyl-1H-pyrrol- 1-yl)acetic acid is used as a bifunctional coupling reagent in the reaction with isonitriles and amines to furnish the target structures. The reaction can be automated and is amenable to library production. The novel synthetic approach described herein can be elaborated further for the synthesis of a wide number of heterocycle-fused 6-oxopiperazine-2-carboxamides.
No preview · Article · Jan 2005 · Heterocyclic Communications