《Table 1 Optimization of reaction conditionsa》

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《原位Cu(Ⅰ)催化的叠氮-炔环加成反应合成长链双功能分子：蓝萼甲素与生物素的长链轭合分子的制备（英文）》

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Initially，the click reaction of biotin-azide 1a and GLA-alkyne 2a was chosen as a model to optimize the reaction conditions.The Cu（I）catalyst system was prepared in advance by mixing CuSO4 and sodium ascorbate in water，and the molar ratio of CuSO4/sodium ascorbate/H2O was 1∶1.5∶0.5.The catalyst system presented as a yellow suspension.The Cu（I）catalyst system was applied to the click reaction under N2 at room temperature.The reactions in mixed solvents such as Et OH-H2O，THF-H2O，tBu OH-H2O（Table 1，Entry 1）with low solubility of substrates shown the negative results.The increased loading of Cu（I）catalyst did not work（Table 1，Entry 2），and more，the ligand of Cu（I），diphenyl disulfide（DPDS）did not promote the reaction（Table 1，Entry 3）.