Peptide therapeutics are an attractive alternative to their small molecule drug counterparts . With several high revenue peptide drugs on the market and a pipeline full of potential candidates , the demand for highly robust and efficient synthetic methods is of great importance. Microwave assisted SPPS has established itself as the primary chemical method to produce high quality peptides while drastically reducing synthesis time and waste . In this presentation, the most recent advances in microwave assisted SPPS are reported. Topics include: (1) unpublished research in the development of a highly active, universal resin for preparing C-terminal peptide acids and (2) a protocol for scale up production using microwave assisted SPPS for the synthesis of peptides in pre-clinical and early phase studies. This protocol incorporates 24 – 48 amino acids per 24hr with a demonstrated scale of 500g purified peptide. Crude purity from R&D to production scale is preserved if not improved and unwanted side reactions such as epimerization and aspartimide formation are easily controlled. The result, easier purification and reduced labor cost.
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