Expeditious and scalable preparation of a Li-Thiele reagent for amine-based bioconjugation
- Resource Type
- Academic Journal
- Authors
- Jiacheng Li; Yuyong Ma; Xiang Zhang; Xin Cao; Hegui Gong; Ang Li
- Source
- 中国化学快报(英文版) / Chinese Chemical Letters. 32(2):700-702
- Subject
- Amine-based bioconjugation
Li Thiele reagent
Arene synthesis
Ortho-phthalaldehyde
- Language
- Chinese
- ISSN
- 1001-8417
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.