Cyclic peptides offer improved stability and bioavailability but require precise cyclization strategies and specialized synthetic techniques to maintain biological activity. The key challenges in this program included:

• Scale and speed – Synthesizing 200+ complex cyclic peptides within tight timeframes.

• Non-canonical amino acids – Incorporating complex, customized amino acids requiring pre-synthesis before SPPS.
• Synthetic difficulties – Managing stereochemistry, ring strain, racemization, and diketopiperazine formation.
• Purification bottlenecks – Processing crude peptides (<5% purity) to final products (≥95% purity) efficiently.

We applied a tailored chemistry and purification strategy, ensuring efficiency at every step:

• Resin selection expertise – Chose optimal resins based on peptide properties for high synthetic efficiency.
• Optimized cyclization – Selected the best approach (on-/off-resin) to maximize yield and purity.
• Cross-functional collaboration – Chemists and purification specialists worked closely to streamline workflows.

We implemented a comprehensive synthetic and purification workflow to efficiently produce high-quality cyclic peptides:

1. Customized SPPS strategy – Automated for routine peptides, manual for challenging sequences.

1. Diverse cyclization techniques – Including click reactions, alkylations, and on-resin modifications.
2. Mitigating synthetic hurdles – Adapting conditions to overcome racemization and ring strain issues.
3. Integrated purification process – Rapid transition from crude peptides to purified compounds meeting biological testing standards.

By combining chemistry expertise with process efficiency, we delivered over 200 high-quality cyclic peptides, accelerating drug discovery efforts:

• 200+ peptides delivered in 8 months – Meeting all project deadlines.
•  ≥95% purity achieved – Through streamlined purification strategies.
•  Seamless incorporation of non-canonical amino acids – Overcoming synthesis challenges.

One-week turnaround per peptide – Enabled by optimized workflows and close team collaboration.