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Despite their high selectivity and low toxicity compared to their small molecule counterparts, a pressing problem when looking at the design of peptide drugs is their poor oral bioavailability and short in vivo half-life. Significant progress has been made to address the disadvantages of peptide drugs through modifications such as head-to-tail cyclization, backbone N-methylation, and “stapling” through a ring-closing metathesis (RCM) reaction, all of which can increase the synthetic difficulty. The application of heat represents an additional tool to optimize the production of challenging synthetic peptides, and a new heating technology, induction heating, has been introduced on the Prelude X. Induction heating allows for independent, simultaneous and rapid heating of multiple reactors with increased efficiency. Different heating conditions, at 25°C, 60°C and 90°C were used for the synthesis of the difficult JR(1-10)peptide (Figure 1) [1].

Multi-Variable Individual Heating Conditions Tested in Parallel Provide Rapid Process Optimization on the Prelude® X