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| Main Authors: | , , , , , |
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| Format: | Artículo Open Access |
| Published: |
Wiley
2026
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| Subjects: | |
| Online Access: | https://onlinelibrary.wiley.com/doi/10.1002/psc.70096 |
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Table of Contents:
- Hydrophobic Tag‐Assisted Scalable Synthesis of Trofinetide and Its GPE Analogues Veeranjaneyulu Avula Sai Krishna Vangapelly Yamanappa Mang S. Umamaheshwar Nagendra Govindappa H. Surya Prakash Rao Journal of Peptide Science ABSTRACT Trofinetide (H‐Gly‐α‐MePro‐Glu‐OH), an FDA‐approved drug for Rett syndrome, is a modified derivative of the neuroprotective tripeptide glypromate (H‐Gly‐Pro‐Glu‐OH; GPE). We report a scalable, high‐yielding liquid‐phase peptide synthesis (LPPS) route employing (2,4‐bis(octadecyloxy)phenyl)methanol (Tag‐OH) as a hydrophobic auxiliary. The method is compatible with both linear and convergent paradigms, with process mass intensity (PMI) analysis confirming the superior efficiency of the convergent approach. In addition to establishing a robust process for trofinetide, the strategy enabled synthesis of two novel non‐natural GPE analogues, H‐Gly‐Aib‐Glu‐OH and H‐Gly‐Aib‐Asp‐OH. This tag‐assisted LPPS provides a greener alternative to existing routes and offers a versatile platform for industrial production of short‐chain oligopeptides. 10.1002/psc.70096 http://onlinelibrary.wiley.com/termsAndConditions#vor