Facile preparation of an orthogonally protected, pH-sensitive, bioconjugate linker for therapeutic applications.
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).
Fletcher
Steven
S
Department of Chemistry, Imperial College Genetic Therapies Centre, Imperial College London, Armstrong Road, London SW7 2AZ, UK.
Jorgensen
Michael R
MR
Miller
Andrew D
AD
D006863:Hydrogen-Ion Concentration; D008298:Maleates / Q000737:chemistry*; D015394:Molecular Structure; D010743:Phospholipids / Q000737:chemistry
D008298:Maleates; D010743:Phospholipids; C030272:maleic acid