概述
N-苄氧羰基-L-高丝氨酸 是带有 N-Carbobenzoxy 保护基团的 L-homoserine,可作为连接子 (ADC Linker) 用于合成抗体药物偶联物 (Antibody-Drug Conjugates (ADCs))。
医药
合成路线 1(1. 合成:35677-88-4)
产率:87.5%
合成条件:With sodium hydrogencarbonate In 1,4-dioxane; water at 20℃;
实验步骤:将L-高丝氨酸(4.76g,40mmol)溶解在H 2 O / 1,4-二恶烷(200mL / 50mL)中。 向混合物中加入NaHCO 3(13.44g,160mmol),加入氯甲酸苄基酯(6.76mL,48mmol)。 将混合物在室温下搅拌过夜。 将混合物用EA洗涤两次。 用HCl(4mol / L)将水层中和至pH 2,用EtOAc萃取1-1。 将合并的有机层用水和盐水洗涤,用无水Na 2 SO 4干燥,蒸发至干。 将残余物1-1不经进一步纯化用于下一步骤(8.86g,35mmol,87.5%)。
参考文献:
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