医药索非布韦中间体;化学合成及生命科学领域原料;作为氨基酸衍生物易被植物吸收,不留残毒,不污染水源,伴有促进植物生长的作用,对农作物有增产效果;应用于食品、化妆品时,代谢产物无常见抗菌剂副作用,可提供营养成分,保护人体健康。
医药; 生命科学; 农业; 食品; 化妆品
路线1:直接酯化法
- 步骤:向装有机械搅拌器、回流冷凝器、温度计和氮气氛的烧瓶中加入(L)-丙氨酸(5.0g,56.1mmol)和氯化氢异丙醇溶液(11.1%w/w,73.8g,224.5mmol),加热至80-85℃反应4小时;TLC(7:3乙醇-水,茚三酮显色)确认转化完成后,真空浓缩除去异丙醇,残余物用乙酸异丙酯多次共蒸发,得产物9.4g。
- 条件:80-85℃;4h;惰性气氛。
- 收率:100%。
- 参考文献:[1] Patent: WO2016/151542, 2016, A1. Location in patent: Page/Page column 19 [2] European Journal of Organic Chemistry, 2018, vol. 2018, # 20, p. 2622-2628 [3] ACS Medicinal Chemistry Letters, 2016, vol. 7, # 12, p. 1197-1201 [4] Patent: WO2015/38596, 2015, A1. Location in patent: Page/Page column 237; 238 [5] Patent: WO2016/145142, 2016, A1. Location in patent: Page/Page column 287 [6] Patent: WO2017/106710, 2017, A1. Location in patent: Page/Page column 77 [7] Patent: WO2017/155923, 2017, A1. Location in patent: Page/Page column 152 [8] Patent: WO2016/30335, 2016, A1. Location in patent: Page/Page column 50 [9] Patent: CN107405356, 2017, A. Location in patent: Paragraph 0210; 0211; 0212 [10] Molecular Pharmaceutics, 2010, vol. 7, # 6, p. 2349-2361 [11] Nucleosides, Nucleotides and Nucleic Acids, 2001, vol. 20, # 4-7, p. 621-628 [12] Patent: US2014/248242, 2014, A1. Location in patent: Paragraph 0361; 0366 [13] Patent: WO2015/107451, 2015, A2. Location in patent: Page/Page column 7 [14] Patent: WO2015/107451, 2015, A3. Location in patent: Page/Page column 7 [15] Patent: WO2017/189978, 2017, A1. Location in patent: Page/Page column 316