Peptide drugs have garnered much attention in recent years. However, conventional peptide synthesis requires an excess amount of expensive reagents of low atom economy, and the large amount of waste produced by these reagents complicates the purification of desired peptides. Solid-phase approaches simplify the purification of these peptides, but these require expensive solid-phase, excess amounts of reagents, substrates, and solvents. This makes it important to develop high-yielding, cost-effective, and less wasteful synthetic approaches. Micro-flow technology (reaction space ≤1 mm) has produced many advantages over conventional batch synthesis. The advantages include precise control of short reaction time and temperature, high levels of light penetration efficiency, lowered risks of handling dangerous compounds, and ready scale-up with high reproducibility. Micro-flow peptide syntheses using these advantages have been reported in recent years. This review summarizes the solid-phase and solution-phase syntheses of α- and β-peptides and of cyclic peptides using micro-flow technology.
Keywords: NCA; cyclic peptide; flow; α-peptide; β-peptide.
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