StratoSpheres for Peptide Synthesis | Agilent
But, whichever cleavage reagent is preferred, it has to be washed out very carefully after Fmoc removal, the last washing must be neutral. When synthesizing large peptides the duration of Fmoc cleavage should be gradually increased. For safe removal of the deblocking reagent the resin may have to be washed more often.
Preloaded Resins for Fmoc Peptide Synthesis:
In peptide synthesis diketopiperazine formation is a notorious side-reaction at the dipeptide stage and is particularly prone to occur in Fmoc based SPPS because of its mechanism.
Rink Amide AM resin and Rink Amide MBHA resin are the most popular resins for the synthesis of peptide amide by Fmoc chemistry. Coupling of the first Fmoc amino acid to the resin can be achieved using the same protocol as for the solid phase peptide synthesis. Detachment of peptide amides from these supports can be effected in a single step by treatment with 95% TFA and appropriate scavengers.
Preloaded Resins for Fmoc Peptide Synthesis
The other approach is to introduce backbone protecting groups which will prevent the formation of hydrogen bonds. Such protection is made by the introduction of the Hmb group on the αnitrogen . It has been shown that the presence of a Hmb unit every 6-7 residues is sufficient to disrupt the peptide aggregation . The Hmb protected amino acid is introduced under the form of N,O-bis-Fmoc-N-(2hydroxy-4-methoxybenzyl) derivative, the O-Fmoc protection being cleaved during the following piperidine treatment. At the end of the synthesis the Hmb group is cleaved in the final TFA cleavage.
Soft shell resins for solid-phase peptide synthesis
A range of cleavage reagents for peptides synthesized on 2-chlorotrityl resin has been described. TFE/AcOH/DCM (1:1:3) has been developed by Barbs . Cleavage is also rapidly attained with 0.5% TFA/DCM as well as with HFIP/DCM (1:4 or 3:7) .