Orthogonal regioselective synthesis of folic acid γ-conjugates

Connelly, Ciera F. and Chow, Shiao Y. (2025) Orthogonal regioselective synthesis of folic acid γ-conjugates. Organic Letters, 27 (49). pp. 13492-13497. ISSN 1523-7060 (https://doi.org/10.1021/acs.orglett.5c04256)

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Abstract

γ-Folic acid conjugates are valuable tools for targeting the folate receptor, an important cancer biomarker, but direct conjugation of folic acid is hampered by poor regioselectivity and challenging purification. We report an orthogonal protection strategy that enables controlled regioselective access to γ-folic acid conjugates from readily available building blocks. This approach permits site-selective installation of a range of functional modalities, including an amphiphilic ligand, a fluorescent probe, and a bioorthogonal handle, followed by global deprotection to afford γ-conjugates without the need for reversed phase chromatography. This publication is licensed u

ORCID iDs

Chow, Shiao Y. ORCID: https://orcid.org/0000-0002-3600-0497

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• Item metadata

  Item type:	Article
  ID code:	94836
  Dates:	Date Event 12 December 2025 Published 27 November 2025 Published Online 19 November 2025 Accepted
  Subjects:	Science > Chemistry
  Department:	Faculty of Science > Pure and Applied Chemistry
  Depositing user:	Pure Administrator
  Date deposited:	27 Nov 2025 12:05
  Last modified:	02 Feb 2026 08:25
  URI:	https://strathprints.strath.ac.uk/id/eprint/94836