Scalable Hydrophobic Tag-Assisted Convergent Synthesis of Cetrorelix Acetate
Abstract
We report a scalable and operationally simple synthesis of cetrorelix acetate, a clinically used decapeptide GnRH antagonist (Ac-D-2′Nal 1 -D-(4-Cl)Phe 2 -D-3′Pal 3 -Ser 4 -Tyr 5 -D-Cit 6 -Leu 7 -Arg 8 -Pro 9 - d -Ala 10 -NH 2 ) employed in in vitro fertilization (IVF) regimens. The peptide was assembled through a convergent [5-mer +5-mer] strategy using tailor-made hydrophobic tags to facilitate fragment anchorage and handling. Pentapeptide intermediates and the final product were constructed via iterative Fmoc-based couplings of suitably protected amino acids. The hydrophobic tags enabled efficient, chromatography-free isolation of intermediates through precipitation and liquid–liquid extraction. This approach provides a practical and scalable route to cetrorelix acetate and demonstrates the utility of tag-assisted peptide synthesis for complex therapeutic peptides.
Fields of Study & Subjects
Chemical Synthesis and Analysis
Click Chemistry and Applications
Biochemical and Structural Characterization
Publication details
- Journal / source
- Organic Process Research & Development
- Publisher
- American Chemical Society (ACS)
- Volume
- 30
- Issue
- 2
- Pages
- 304–311
- Publication date
- 23 January 2026
- Language
- EN