The Chan-Lam-type synthesis of thioimidazolium salts for thiol-(hetero)arene conjugation
Yue Li,
Dongchang Han,
Zhibin Luo
et al.
Abstract:The design of stable and variable aryl linkers for conjugating drug moieties to the metabolism-related thiols is of importance in drug discovery, especially in the field of antibody-drug conjugates (ADCs). We disclosed that thioimidazolium groups are unique scaffolds for the thiol-(hetero)arene conjugation under mild conditions. The drug bound thioimidazolium salts, which are easily accessible via a copper-mediated Chan-Lam process in gram-scale, could be successfully applied to the late-stage coupling of bioa… Show more
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