Expeditious and scalable preparation of a Li-Thiele reagent for amine-based bioconjugation

• 来源期刊: 中国化学快报（英文版）
• 年，卷（期）: 2021,（2）
• 所属期刊栏目: Communications
• 页码范围: 700-702
• 页数: 3页
• 语种: 英文

摘要

Chemoselective amine bioconjugation has long been a challenge for native protein modification.Inspired by Thiele's seminal discovery,Li and co-workers recently developed an ortho-phthalaldehyde (OPA) based reagent for labeling the amino group of a protein.Here we report an expeditious and scalable synthesis of a Li-Thiele reagent featuring an arene construction strategy.The reagent contains an alkyne side chain as a handle for secondary modification.