A Scalable Strategy for Peptide Diversification Using N-Betsylated Amino Acids

Access to noncanonical amino acids is critical for expanding peptide chemical space, but traditional approached can limit opportunities for late-stage modification and diversification. This poster showcases a practical, scalable route to N-betsylated amino acids that enables peptide functionalization, macrocyclization, and diversification while remaining compatible with standard SPPS workflows.

Learn how Sygnature Discovery developed a sulfinate-hypochlorite approach to synthesized N-betsylated amino acids using inexpensive, readily available reagents. The poster highlights:

• Scalable synthesis of N-betsylated amino acids
• Broad compatibility across canonical amino acids
• SPPS-compatible peptide modification strategies
• Applications in peptide macrocyclization
• On-resin and liquid-phase N-functionalization
• New opportunities for late-stage peptide diversification

Advancing Peptide Discovery

The Bts group serves as a versatile orthogonal handle for peptide modification, enabling transformations that are difficult to achieve using conventional peptide synthesis approaches. This work expands Sygnature Discovery’s peptide toolbox and supports rapid generation of structurally diverse peptide therapeutics for drug discovery programs.