化学合成。
化学合成
合成路线 1(1. 合成:7170-36-7)
产率:87%
合成条件:With potassium hydroxide In methanol at 20℃;
实验步骤:向20(10.0g,51.2mmol)的MeOH(300mL)溶液中加入KOH(2.89g,51.2mmol)并将混合物在室温下搅拌过夜。 除去溶剂后,将残余物用水稀释。 用AcOEt洗涤水层并用浓盐酸酸化。 用HCl水溶液,然后用CHCl3 /异丙醇(3/1(v / v))溶液萃取混合物。 将有机层用MgSO 4干燥并真空浓缩,得到21(8.17g,87%),为白色固体。
参考文献:
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合成路线 2(3. 合成:7170-36-7)
产率:65%
合成条件:With N-ethyl-N,N-diisopropylamine In tetrahydrofuran for 4 h; Reflux
实验步骤:一般合成程序如下。 将吡啶-2,6-二羧酸(1,1.5g,8.98mmol)与24mL SOCl 2混合。 将得到的混合物回流3小时。 然后在真空下除去过量的SOCl2。 向2的白色固体中加入50mL THF。 固体溶解后,用注射器加入烷基醇(10.5mmol)和DIEA(10.5mmol)。 使所得溶液回流4小时。 除去溶剂后,将残余物应用于色谱法,得到所需产物3和4。
参考文献:
- [1] Tetrahedron, 2011, vol. 67, # 44, p. 8458 - 8464