作为烷基二胺类化合物,利用结构中两个氨基单元的亲核性,用于蛋白降解靶向嵌合体(PROTAC)分子的连接体;也可用于化学合成。
化学合成;生物化学基础研究(PROTAC分子连接体)
合成路线 1(2752-17-2)
- 原料:15(575mg,0.83mmol)和80%水合肼(8.3mmol)
- 溶剂:氯仿(CHCl₃,10mL)
- 步骤:将原料与水合肼在氯仿中混合,回流搅拌4小时;反应完成后用水处理,氯仿萃取,有机层用MgSO₄干燥,蒸发溶剂后蒸馏纯化
- 条件:回流(Reflux)4小时
- 产率:93%
- 产物表征:bp 75-79°C / 5 mmHg(文献值:bp 55-60°C / 2 mmHg);¹H NMR(500MHz,DMSO-d6)δ 8.31(4H,br s),3.32(4H,t,J=5.5Hz),2.63(4H,t,J=5.5Hz);¹³C NMR(500MHz,DMSO-d6)δ 72.7, 41.3;MS(FAB)m/z:105 [M+H]
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