5-氨基异酞酸单甲酯是一种中间体,用于医药相关化合物的合成(如专利WO2009/15166中提及的联苯类衍生物合成)。
医药
合成路线 1(1. 合成:28179-47-7)
产率:92%
合成条件:With hydrogen In methanol for 5 h;
实验步骤:实施例14 5 - ((1R,2S)-2 - ((S)-4-(4-氯苯基)-4-羟基-3,3-二甲基哌啶-1-羰基)环己基氨基甲酰基)联苯-3-甲酸甲酯5步骤1: 3-氨基-5-(甲氧基羰基)苯甲酸的制备将20%Pd(OH)2(0.50g)在氩气下用甲醇(5mL)小心地润湿,然后用3-(甲氧基羰基)-5-硝基苯甲酸润湿。 加入(5.00g,22.2mmol)的甲醇(20mL)溶液。 然后将混合物在Parr Shaker装置上在50psi下氢化5小时。 在氩气下,通过玻璃纤维滤纸小心地过滤反应。 浓缩滤液,得到3-氨基-5-(甲氧基羰基)苯甲酸(4.0g,20.5mmol,92%收率)灰白色固体产物。 MS发现:(M - H)+ = 194。
参考文献:
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