生命科学;化学合成,医药阿扎那韦中间体。N-甲氧羰基-L-叔亮氨酸可作为有机合成中间体和医药中间体,主要用于实验室研发和化工生产过程中。制备:在L-丙氨酸(8 g, 168 mmol)的1N NaOH (168 mL)溶液中加入Na₂CO₃ (8.9 g, 84 mmol)。将溶液冷却至0°C,逐滴加入氯甲酸甲酯(20.5 mL, 172 mmol)。反应混合物在室温下搅拌3.5小时。溶液用Et₂O洗涤,用1N HCl酸化至pH约为1。水层用DCM提取,有机层用盐水洗涤,用Na₂SO₄干燥,浓缩得到目标中间体N-甲氧羰基-L-叔亮氨酸。
医药中间体;有机合成中间体
路线1:
- 步骤:(S)-2-氨基-3,3-二甲基丁酸的搅拌溶液(约5.0g,38.6mmol)在约0℃下,在二恶烷(约20ml)和氢氧化钠(2N,62ml,PH=8-9)中,逐滴加入甲基氯代甲酸酯(约5.88ml,76.33mmol)并在约60℃下搅拌。大约18个小时。将反应混合物冷却至室温,用DCM萃取,分离水层并用1N HCl酸化。将所得溶液用EtOAc萃取,经Na₂SO₄干燥,并在减压下蒸发溶剂。将所得粗产物在己烷中搅拌并蒸馏,得到标题化合物,为固体。
- 条件:With sodium hydroxide In 1,4-dioxane; water at 60℃; for 18 h;
- 产率:100%
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