化学合成,医药中间体;用于有机合成,也用作医药中间体;用于心血管药物依替米贝的合成;伊泽替米贝中间体。
医药
路线1:
- 步骤: 在0℃下向搅拌的氯化铝(205.85g,1.54MOL)在二氯甲烷(500ML)中的悬浮液中加入戊二酸酐(80g,0.7MOL)二氯甲烷(125ML)的溶液。将反应物料搅拌30分钟,并将氟苯(67.36g,0.7MOL)缓慢加入反应物料中。通过TLC监测反应完成,然后在搅拌下倒入冰冷的水(2000ML)中,过滤收集分离的固体。将固体溶于3%氢氧化钠水溶液(1100ML)中并用二氯甲烷(300ML)洗涤。将水层酸化,得到沉淀物。过滤固体,用水洗涤,真空干燥,得到标题产物(125g,收率:85%)。
- 条件: at 0℃; for 0.50 h
- 产率: 85%
- 参考文献: [1] Patent: WO2004/99132, 2004, A2. Location in patent: Page 7-8 [2] Bioorganic and Medicinal Chemistry Letters, 2010, vol. 20, # 15, p. 4424 - 4426 [3] Patent: CN106397292, 2017, A. Location in patent: Paragraph 0053; 0083; 0084 [4] Patent: US2006/135755, 2006, A1. Location in patent: Page/Page column 15 [5] Patent: EP1137634, 2005, B1. Location in patent: Page/Page column 9 [6] Tetrahedron, 1993, vol. 49, # 15, p. 3193 - 3202 [7] Tetrahedron Letters, 2016, vol. 57, # 10, p. 1079 - 1082 [8] Patent: WO2003/104180, 2003, A1. Location in patent: Page 6-8 [9] Patent: WO2003/104180, 2003, A1. Location in patent: Page 9 [10] Patent: WO2007/17705, 2007, A1. Location in patent: Page/Page column 12 [11] Patent: US2015/18565, 2015, A1. Location in patent: Paragraph 0035; 0036; 0037 [12] Patent: US2016/280642, 2016, A1. Location in patent: Paragraph 0056 [13] Patent: CN103694111, 2016, B. Location in patent: Paragraph 0032-0035; 0042 [14] Chirality, 2018, vol. 30, # 5, p. 642 - 651