作为含氟哌啶类医药中间体,用于相关药物分子的合成。
医药
合成路线 1(1. 合成:211108-50-8)
产率:99%
合成条件:With Selectfluor In acetonitrile at 20 - 40℃; for 2.16 h;
实验步骤:步骤B:3-氟-4-氧代哌啶-1-羧酸叔丁酯的制备: 在环境温度下,向4-(三甲基甲硅烷基氧基)-5,6-二氢吡啶-1(2H) - 羧酸叔丁酯(64.4g,237mmol)的无水ACN(1.5L)溶液中加入Selectfluor(92.5g,261)。 在10分钟内分批分离,在此期间观察到轻微的放热(至40℃)。 将混合物搅拌2小时,然后浓缩至干,并在EtOAc和盐水之间分配。 水层用EtOAc萃取,合并的有机相用盐水洗涤,用Na 2 SO 4干燥,过滤并浓缩,得到51g(99%)所需产物,为固体。
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