LINKER STRATEGIES IN MODERN SOLID-PHASE ORGANIC SYNTHESIS

LINKER STRATEGIES IN MODERN SOLID-PHASE ORGANIC SYNTHESIS 

Solid-Phase Organic Synthesis Concepts, Strategies, and Applications, First Edition. Edited by Patrick H. Toy and Yulin Lam. 

Out of the combinatorial chemistry boom came the framework for modem solid-phase organic synthesis. While a lot of the early work with SPOS focused on reliable and relatively straightforward peptide coupling reactions, the ambitious library syntheses of the 1990s required access to a much more extensive array of solid-phase reactions. That decade saw initial strides made in adapting many well-known solution-phase reactions for use in the solid-phase arena, development that continues to the present day, and a move beyond peptide and nucleotide chemistry toward preparation of small molecule libraries on solid phase. 

In time, the vast libraries of combinatorial chemistry have given way to the smaller designed libraries of diversity-oriented synthesis (DOS). Rather than preparing multimillion compound libraries in the hope of finding new lead scaffolds, DOS concentrates on 

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