作为有机合成中间体，广泛应用于医药领域的相关化合物合成。
医药
合成路线 1（1. 合成：144072-29-7）
- 步骤: 向对氨基-苯甲醇（1g，8.12mmol，1当量）在80mL无水THF中的溶液中加入DIEA（1.4mL，8.12mmol，1当量）和Boc₂O（1.9mL，8.12mmol，1当量）；将混合物加热至回流过夜，冷却并真空蒸发；残余物溶于EtOAc，用0.1N HCl洗涤，MgSO₄干燥，过滤并真空蒸发；硅胶柱色谱（Hex-EtOAc，1:1）纯化得产物。
- 条件: With N-ethyl-N,N-diisopropylamine In tetrahydrofuran; Heating / reflux
- 产率: 100%
- 参考文献: [1] Patent: WO2008/34124, 2008, A2. Location in patent: Page/Page column 72-73 [2] Patent: WO2006/31806, 2006, A2. Location in patent: Page/Page column 99 [3] Research on Chemical Intermediates, 2017, vol. 43, # 3, p. 1355 - 1363 [4] Tetrahedron Letters, 2007, vol. 48, # 51, p. 9044 - 9047 [5] Journal of Medicinal Chemistry, 1992, vol. 35, # 22, p. 4150 - 4159 [6] Organic and Biomolecular Chemistry, 2006, vol. 4, # 7, p. 1305 - 1312 [7] Patent: WO2008/127349, 2008, A2. Location in patent: Page/Page column 103 [8] Patent: WO2015/26990, 2015, A2. Location in patent: Page/Page column 44; 45 [9] Patent: WO2015/144933, 2015, A1. Location in patent: Page/Page column 33; 34 [10] Patent: WO2017/66668, 2017, A1. Location in patent: Paragraph 000218-000221 [11] Tetrahedron Letters, 2010, vol. 51, # 33, p. 4371 - 4374 [12] Bioorganic and Medicinal Chemistry, 2017, vol. 25, # 12, p. 3018 - 3033 [13] Journal of Medicinal Chemistry, 2015, vol. 58, # 23, p. 9354 - 9370 [14] Journal of Medicinal Chemistry, 1989, vol. 32, # 4, p. 811 - 826 [15] Bioorganic and Medicinal Chemistry Letters, 2003, vol. 13, # 24, p. 4293 - 4297 [16] Journal of Medicinal Chemistry, 2004, vol. 47, # 10, p. 2411 - 2413 [17] Patent: US2004/157900, 2004, A1. Location in patent: Page 5 [18] Patent: US2003/153752, 2003, A1 [19] Patent: US2003/153752, 2003, A1 [20] Patent: US2004/77646, 2004, A1. Location in patent: Page 93 [21] Chemistry of Materials, 2011, vol. 23, # 21, p. 4844 - 4856 [22] Bioorganic and Medicinal Chemistry, 2017, vol. 25, # 14, p. 3614 - 3622
合成路线 2（一般步骤）
- 步骤: 在氮气保护下，将对氨基苯甲醇（1g，8.12mmol，1当量）溶解于80mL无水THF中；依次加入DIEA（1.4mL，8.12mmol，1当量）和Boc₂O（1.9mL，8.12mmol，1当量）；加热至回流并搅拌过夜；冷却至室温，旋转蒸发浓缩；残余物溶于EtOAc，0.1N HCl洗涤，MgSO₄干燥，过滤后减压浓缩；硅胶柱色谱（石油醚-乙酸乙酯1:1）纯化得产物。
- 条件: 氮气保护；加热回流；无水THF；DIEA；Boc₂O
- 产率: 100%
- 参考文献: [1] Patent: WO2008/34124, 2008, A2. Location in patent: Page/Page column 72-73 [2] Patent: WO2006/31806, 2006, A2. Location in patent: Page/Page column 99 [3] Research on Chemical Intermediates, 2017, vol. 43, # 3, p. 1355 - 1363 [4] Tetrahedron Letters, 2007, vol. 48, # 51, p. 9044 - 9047
