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Solid Phase Peptide Synthesis, 2nd ed.

The head-to-tail on-resin cyclization strategy is an important tool in solid phase peptide synthesis that takes advantage of the resin-induced pseudo-dilution effects, thereby limiting undesirable dimerization.

Quantitative monitoring of solid‐phase peptide synthesis by the ninhydrin reaction.

The UV monitoring feature also allows the synthesis conditions to be modified in situ, so the system automatically repeated the Fmoc removal step to achieve full deprotection.

Protein Engineering: Design and synthesis of a protein.

While the early work in this field focused on applying microwave energy only to the coupling reaction, the scope of microwave technology as a tool for enhancing peptide synthesis now covers the entire process, including both the coupling and deprotection reactions, as well as the post-synthesis cleavage step to remove the peptide from the resin and remove the side chain-protecting groups.

In the case of this 10-mer peptide, 15-minute double couplings were selected, which in addition to the ancillary deprotection step, improved the synthesis quality to 88% with minimal deletions observed.

Solid-phase synthesis of peptide …

It was not long after this seminal work that peptide chemists were using microwave technology to improve the solid-phase synthesis of more complex biomolecules.

The peptide backbone (Gly-Val-Tyr-Leu-His-Ile-Glu) was synthesized on Fmoc-Glu(Wang resin)-ODmab with the side chain γ-carboxyl group anchored to the resin and the α-carboxyl protected by the Dmab orthogonal protecting group in 91% crude purity.

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