生命科学,选择性环氧合酶-2抑制剂。
医药
合成路线 1(1. 合成:1601-18-9)
产率:84%
合成条件:Stage #1: With bis-(2-oxo-3-oxazolidinyl)phosphoryl chloride; triethylamine In dichloromethane for 0.17 h; Inert atmosphere Stage #2: for 12 h; Inert atmosphere
实验步骤:通用方法:将吲哚美辛(1eq。)和BOP-Cl(1eq。)悬浮在二氯甲烷(20mL / g酸)中,缓慢加入NEt 3(2eq。)并将混合物搅拌10分钟。 加入相应的醇(4eq。,1eq。,2i),将混合物搅拌至少12小时。 蒸发溶剂,通过柱色谱法用己烷(80-100℃)和乙酸乙酯(3:1)的混合物纯化固体。 减压除去溶剂,得到相应的酯,为浅黄色固体。
参考文献:
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