Two Facile General Methods for the Conjugation of Three Different Molecules

摘要

In the quest to synthesize compounds that are uniquely optimized for fighting each individual target disease,the importance of developing a new methodology for the bioconjugation of compounds with different functional groups or biological activities cannot be overemphasized.This study investigates two novel methods for click reaction: coupling a molecule with three functional compounds by repetitive copper(I)catalyzed azide/alkyne 1,3-dipolar cycloadditions.Method A uses three copper(I)catalyzed azide/alkyne 1,3-dipolar cycloadditions in series.Method B uses two copper(I)catalyzed azide/alkyne 1,3-dipolar cycloadditions and one conjugation reaction of amine and isothiocyanate.