作为医药中间体,用于相关药物分子的合成。
医药中间体
合成路线 1(1. 合成:95656-86-3)
产率:100%
合成条件:With N-ethyl-N,N-diisopropylamine In methanol at 20℃;
实验步骤:步骤1:向1-氨基 - 丙-2-醇(化合物42.1; 3.53g,47.0mmol)和TEA(25mL)的MeOH(35mL)混合物中缓慢加入二碳酸二叔丁酯溶液 (10.3g,47.0mmol)的MeOH(15mL)溶液。 将所得溶液在室温下搅拌过夜。 然后浓缩混合物,残余物在高真空下干燥,得到8.23g(定量)透明油状物。 将由此获得的油状物溶于THF(100mL)中并用TEA(13.1mL,94.0mmol)处理。 在氮气下,在0℃下向所得溶液中滴加甲磺酰氯(0.3.82mL,49.3mmol)。 1小时后,将混合物用EtOAc稀释,并用1M HCl水溶液,碳酸氢钠水溶液和盐水洗涤。 将有机相干燥(Na 2 SO 4)并浓缩,得到10.5g(88%)透明油状的(化合物42.2),其在静置时固化,ES(+)MS m / e = 254(M + H +)。
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