作为医药中间体,用于合成相关药物分子。
医药
合成路线 1(2. 合成:17012-21-4)
产率:1420 g
合成条件:With trifluoroacetic acid In dichloromethane at 0 - 20℃; Large scale
实验步骤:向250mL多个小瓶中加入1530.0g(6.5mol)苄基甲氧基甲基三甲基甲硅烷基甲胺,31.80g(3.7mol)丙烯酸甲酯和38mL二氯甲烷,44.0g(0.4mol)三氟乙酸的溶液,质量浓度为10% 在0℃下缓慢滴加,滴加完成后,将混合物在室温下搅拌过夜,减压浓缩混合物,残余物分别用饱和碳酸氢钠溶液和饱和氯化钠溶液洗涤,合并 有机相,有机相经无水硫酸钠干燥,过滤,滤液减压浓缩,得到1420.0g粗品1-苄基吡咯烷-3-羧酸酯,为粗产物100%。
参考文献:
- [1] Bioorganic and Medicinal Chemistry Letters, 2004, vol. 14, # 19, p. 4861 - 4866 [2] Organic Process Research and Development, 2009, vol. 13, # 2, p. 292 - 296 [3] Synthesis, 2006, # 16, p. 2646 - 2648 [4] Synlett, 2015, vol. 26, # 13, p. 1815 - 1818 [5] Chemical & Pharmaceutical Bulletin, 1985, vol. 33, # 7, p. 2762 - 2766 [6] Tetrahedron Letters, 2011, vol. 52, # 26, p. 3266 - 3270 [7] Patent: CN104817549, 2017, B. Location in patent: Paragraph 0036-0038