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PreprintCC BYChemRxiv

Efficient Microwave-Enhanced Solid Phase Peptide Synthesis of Secretin Hormones Amenable for Rapid Library Design and Lead Optimization

  • Brenson A. Jassim1,2
  • Kyle T. Faivre2,3
  • Severin T. Schneebeli1,2,3,4,5
5 affiliations
  1. 1Department of Industrial and Molecular Pharmaceutics
  2. 2Institute for Drug Discovery
  3. 3Department of Chemistry
  4. 4Institute of Inflammation, Immunology, and Infectious Disease
  5. 5Purdue University
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Abstract

Microwave-enhanced solid phase peptide synthesis of complex, therapeutically relevant, aspartimide-prone secretin hormones was achieved under optimized conditions with economical and commercially available protected amino acids. In order to determine robust and general methods, standard Fmoc SPPS conditions, Oxyma-buffered deprotection solution, Fmoc-(Dmb)Gly-OH, Fmoc-Asp(OMpe)-OH, and combinations thereof were systematically evaluated for crude purity using LC-MS. Aspartimide formation was significantly reduced, and syntheses were completed in a single run without the need for expensive, commercially inaccessible, or diversity-limiting peptide fragments or pseudoprolines, supplying methods amenable for rapid library generation, hit-to-lead endeavors, and lead optimization.

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Cite

BibTeXRIS
BibTeX
@misc{jassim2026efficient,
  title = {{Efficient Microwave-Enhanced Solid Phase Peptide Synthesis of Secretin Hormones Amenable for Rapid Library Design and Lead Optimization}},
  author = {Brenson A. Jassim and Kyle T. Faivre and Severin T. Schneebeli},
  howpublished = {ChemRxiv},
  year = {2026},
  month = oct,
  doi = {10.26434/chemrxiv.15003792/v2},
  url = {https://chemrxiv.org/doi/full/10.26434/chemrxiv.15003792/v2},
  note = {CC BY},
}
RIS
TY  - UNPB
TI  - Efficient Microwave-Enhanced Solid Phase Peptide Synthesis of Secretin Hormones Amenable for Rapid Library Design and Lead Optimization
AU  - Brenson A. Jassim
AU  - Kyle T. Faivre
AU  - Severin T. Schneebeli
PY  - 2026
DA  - 2026/10/06
PB  - ChemRxiv
DO  - 10.26434/chemrxiv.15003792/v2
UR  - https://chemrxiv.org/doi/full/10.26434/chemrxiv.15003792/v2
AB  - Microwave-enhanced solid phase peptide synthesis of complex, therapeutically relevant, aspartimide-prone secretin hormones was achieved under optimized conditions with economical and commercially available protected amino acids. In order to determine robust and general methods, standard Fmoc SPPS conditions, Oxyma-buffered deprotection solution, Fmoc-(Dmb)Gly-OH, Fmoc-Asp(OMpe)-OH, and combinations thereof were systematically evaluated for crude purity using LC-MS. Aspartimide formation was significantly reduced, and syntheses were completed in a single run without the need for expensive, commercially inaccessible, or diversity-limiting peptide fragments or pseudoprolines, supplying methods amenable for rapid library generation, hit-to-lead endeavors, and lead optimization.
ER  -