Reviews on Linkers in Solid-Phase Synthesis

1 Tracelessness Unmasked A General Linker Nomenclature. Comely, A. C Gibson, S E. Angew. Chenu, Int Ed. 2001, 40,1012-1032. 

2 Biocatalysis in PblymerSupported Synthesis Enzyme-Labile Linker Groups. Reents, R. Jeyaraj, D. A. Waldmann, H. Adv. Synth. Catal 2001,343, 501. 

3 Linkers and Cleavage Strategies in Solid-Phase Organic Synthesis and Combinatorial Chemistry. Guillier, F. Orain, D. Bradley, M. Chem. Rev. 2000, 100, 2091-2157. 

4 Linkers for Solid-Phase Organic Synthesis. James, I. W. Tetrahedron 1999, 55, 4855-4946. 

5 Resins, Linkers, and Reactions for Solid-Phase Synthesis of Organic Libraries. Felder, E. R. In Combinatorial Chemistry and Technology Miertus. S., Fassina, G., Eds. Dekker New York, 1999, pp 35-51. 

---

Reviews on Linkers in Solid-Phase Synthesis 42 Reviews on the Synthesis of Complex Targets Including Discussion of Protecting Group Problems and Strategies 42... 

Over the years, a number of cleavable linkers that are acid labile, base labile, or photol-abile have been developed for solid-phase peptide synthesis. (This topic has been covered in detail by several review papers [34-36].) For libraries that require the linker to be cleaved before screening, most of these conventional linkers can be used. Several unconventional linkers have been found to be particularly useful and user-friendly for combinatorial applications (see Fig. 1). Among them are methionine-containing linker [37] and safety-catch benzylhydrylamine linker 1 [38], Bray et al. [39] have utilized an orthogonal peptide-resin linker 2 which allows the final deprotection and removal of contaminating chemicals and the peptide is later released into an aqueous buffer. Hoffmann and Frank [40] recently described a novel safety-catch linker 3 based on the intramolecular catalytical... 

---