135042-12-5 (2R,4R)-1-(叔丁氧羰基)-4-羟基吡咯烷-2-羧酸

• [1] Patent: WO2014/78609, 2014, A1. Location in patent: Paragraph 00176

合成路线 3（3. 合成：135042-12-5）

产率：91% 合成条件：Stage #1: With sodium hydroxide In tetrahydrofuran; water at 20℃; Stage #2: With hydrogenchloride In water 实验步骤：向5L三颈烧瓶中加入（R，-α）-4-羟基 - 吡咯烷-2-羧酸（300g，2.228mol），二碳酸二叔丁酯（499.3g，2.228mol）。 ，50％（w / w）NaOH（118mL，2.228mol），THF（2L）和H 2 O（1L）。 将反应物在室温下搅拌过夜。 向反应混合物中加入3N HCl（762mL，2.286mol）。 分离有机层和水层。 将盐水（1L）加入水层中，用THF（1L）萃取。 合并有机层，用MgSO 4干燥并浓缩，得到湿饼。 将湿滤饼与己烷（各2L）共沸两次，得到标题化合物，为白色至灰白色固体（469g，91％收率）。 参考文献：

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