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An Inexpensive Adaptation of a Commercial Microwave Reactor for Solid Phase Peptide Synthesis

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Advances in Fmoc solid-phase peptide synthesis.

Raymond Behrendt¹, Peter White², John Offer³

¹Novabiochem, Merck & Cie, Im Laternenacker 5, 8200, Schaffhausen, Switzerland.

Journal of Peptide Science : an Official Publication of the European Peptide Society

|January 21, 2016

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9-fluorenylmethoxycarbonyl solid-phase peptide synthesis (Fmoc SPPS) is the leading method for creating peptides. High-quality Fmoc building blocks are affordable due to large-scale therapeutic peptide production, enabling diverse peptide derivative synthesis.

Area of Science:

Organic Chemistry
Medicinal Chemistry
Biochemistry

Background:

9-fluorenylmethoxycarbonyl solid-phase peptide synthesis (Fmoc SPPS) is the predominant technique for synthesizing peptides.
Economies of scale from multiton therapeutic peptide production have led to low-cost, high-quality Fmoc building blocks.
Commercial availability of numerous modified Fmoc building blocks simplifies the synthesis of diverse peptide derivatives.

Purpose of the Study:

To highlight the current status and advantages of Fmoc SPPS in peptide synthesis.
To underscore the impact of large-scale production on building block accessibility and cost.
To discuss the role of Fmoc SPPS in meeting the growing demands of medicinal chemistry and pharmacology.

Main Methods:

Utilizes Fmoc SPPS chemistry for peptide chain elongation.

Keywords:

Fmoc/tBu aspartimide peptide thioester post-translational modification protecting group racemisation solid-phase peptide synthesis

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Published on: May 15, 2012

Employs commercially available Fmoc-protected amino acid derivatives.

Leverages established solid-phase synthesis protocols.

Main Results:

Fmoc SPPS enables straightforward synthetic access to a wide array of peptide derivatives.
Cost-effectiveness of Fmoc building blocks is driven by large-scale manufacturing.
Continuous improvements in peptide quality, synthesis speed, and target scope are being achieved.

Conclusions:

Fmoc SPPS remains the method of choice for peptide synthesis due to its efficiency and versatility.
Advancements in Fmoc SPPS technology are crucial for supporting the increasing number of synthetic peptides in clinical trials.
Ongoing research in peptide chemistry further expands the applications of Fmoc SPPS.