TOPPA Resins
Figure 1: structure of TOPPA resins: total protected peptide amide.
So far only a few linker are available for the synthesis of completely protected peptide amides1-3. But they suffer so far from complicated handling and high prices. We describe here an easy way by using commercial available linkers for the synthesis of total protected peptide amides.
Available as PS TOPPA and TentaGel® TOPPA.
The Concept
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Resin
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RAM-2ClTrt-polystyrene,100-200 mesh, 0.82 mmol/g
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Chemistry
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Fmoc chemistry, HBTU activation
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Cleavage Conditions
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TFE/HOAc/DCM (2:2:6), 3h
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The Result
References
- B. J. Backes, J. A. Ellmann, J. Am. Chem. Soc.,116, 11171(1994).
- C.P. Holmes, et. al., J. Org. Chem., 60, 2318 (1995).
- P. Sieber, Tetrahedron Lett., 28, 2107(1987).
- D. Gatos, C. Tzavara, J. Pep. Res. 2001, 168-7.