A Sustainable Synthetic Methodology for Peptides and Peptidomimetics

Join guest speakers Fernando Albericio of the Institute for Research in Biomedicine – Barcelona and Christina Schroeder of the University of Queensland Institute of Molecular Bioscience for a lunch included workshop. With Michael J. Karney of CEM Corporation, they will present practical applications data and peer-reviewed research detailing a total synthetic methodology that utilizes microwave energy to provide the best results for peptide purity, production throughput, and use of solvents. This new strategy includes:

• Universal carbodiimide coupling which increases purity and suppresses side reactions such as epimerization and aspartimide formation without the need for step-wise reaction optimization
• One-pot coupling and deprotection process for increased efficiency
• Reduction of up to 95% generated waste compared to conventional methods

This methodology is applied to the synthesis of a number of pharmaceutically relevant sequences (liraglutide, thymosin, beta-amyloid, ubiquitin), challenging structural motifs (N-methylated, glyco/phosphopeptides), and post-synthetically modified peptides (cyclized, stapled, branched) to demonstrate success.