Department of Chemistry, Aarhus University, Aarhus, Denmark.
Org Biomol Chem. 2019 Jul 24;17(29):6970-6974. doi: 10.1039/c9ob01384a.
We demonstrate that an extended scaffold based on a self-immolative linker (SIL) enables the universal production of O-aryl glucuronide prodrugs: high yield glucuronidation is performed on a precursor substrate (SIL) and the subsequent drug conjugation proceeds via less challenging chemical reactions.
我们证明了一种基于自毁连接子（SIL）的扩展支架能够实现 O-芳基葡萄糖醛酸酯前药的通用生产：在前体底物（SIL）上进行高产率的葡萄糖醛酸化，随后通过挑战性较小的化学反应进行药物偶联。
