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We report the total synthesis of a triazole‐epothilone analogue 1. The key step to generate the macrocyclic ring and the triazole ring was to apply Cu2O nanoparticles (Cu2O‐NPs) to catalyze the 1,3‐dipolar cycloaddition. The conformation of 1 and its bioactivity in MCF cancer cell lines were investigated.
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