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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Facile preparation of an orthogonally protected, pH-sensitive, bioconjugate linker for therapeutic applications
Steven Fletcher1, Michael R Jorgensen, Andrew D Miller
1Department of Chemistry, Imperial College Genetic Therapies Centre, Imperial College London, Armstrong Road, London SW7 2AZ, UK.
Organic Letters
|November 5, 2004
Abstract:
We describe the facile, three-step synthesis of an orthogonally protected, pH-sensitive linker (8), based on maleic acid, and report its application to the preparation of a pH-sensitive phospholipid (20) for potential use in drug and gene delivery. In addition, we highlight the benefits of our linker over the use of the commercially available cis-aconitic anhydride (4).

