Improved Methodology for the Synthesis of a Cathepsin B Cleavable Dipeptide Linker, Widely Used in Antibody-Drug Conjugate Research

•A revised synthesis was developed for the Val-Cit linker widely employed in ADCs.•The methodology proved to be high-yielding, reproducible, and devoid of epimerization.•A new drug-linker construct bearing a novel tubulin-active payload was synthesized.