化学合成。
化学合成
合成路线 1（1. 合成：77279-24-4）
产率：100%
合成条件：for 2 h;
实验步骤：4-（2-羟乙基）哌嗪-1-羧酸叔丁酯（57）：向1-（2-羟乙基）哌嗪（3.0g，23.0mmol）的THF溶液中加入二碳酸二叔丁酯（5.5g，25.3） 将混合物搅拌2小时。真空蒸发溶剂至初始体积的一半，将混合物倒入水中，用CH 2 Cl 2萃取，用盐水洗涤，用Na 2 SO 4干燥并浓缩，得到浅黄色油状物（ 5.3 g，quant。）。1H NMR（400 MHz，CDCl3）δ1.46（s，9H），2.44-2.46（m，4H），2.54-2.57（m，2H），2.66（m，J = 5.3， 1H），3.42-3.45（m，4H），3.62（q，J = 5.3,2H）。
参考文献：
- [1] Bioorganic and Medicinal Chemistry, 1997, vol. 5, # 4, p. 693 - 705 [2] Farmaco, 2004, vol. 59, # 12, p. 971 - 980 [3] Patent: US2011/263534, 2011, A1. Location in patent: Page/Page column 89 [4] Journal of Polymer Science, Part A: Polymer Chemistry, 2016, vol. 54, # 8, p. 1098 - 1108 [5] Patent: WO2006/107923, 2006, A1. Location in patent: Page/Page column 66 [6] Patent: WO2017/18805, 2017, A1. Location in patent: Paragraph 714-716 [7] Archiv der Pharmazie, 2003, vol. 336, # 8, p. 372 - 380 [8] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 21, p. 6274 - 6280 [9] Patent: WO2014/174060, 2014, A1. Location in patent: Page/Page column 101 [10] Patent: WO2014/174062, 2014, A1. Location in patent: Page/Page column 74 [11] Patent: WO2015/162293, 2015, A1. Location in patent: Page/Page column 198 [12] Journal of Medicinal Chemistry, 2009, vol. 52, # 19, p. 5974 - 5989 [13] Journal of Medicinal Chemistry, 2007, vol. 50, # 14, p. 3242 - 3255 [14] Patent: US6034127, 2000, A [15] Patent: US5792769, 1998, A [16] Bioorganic and Medicinal Chemistry, 2018, vol. 26, # 23-24, p. 6035 - 6049 [17] Patent: WO2013/64445, 2013, A1. Location in patent: Page/Page column 169 [18] Journal of the Chinese Chemical Society, 2011, vol. 58, # 4, p. 538 - 543 [19] Journal of Medicinal Chemistry, 2010, vol. 53, # 16, p. 6129 - 6152 [20] Chinese Journal of Catalysis, 2013, vol. 34, # 9, p. 1730 - 1733 [21] Patent: WO2013/160810, 2013, A2. Location in patent: Paragraph 0277 [22] Patent: US2009/203695, 2009, A1. Location in patent: Page/Page column 8 [23] Patent: US2009/281087, 2009, A1. Location in patent: Page/Page column 20 [24] Patent: WO2009/147221, 2009, A1. Location in patent: Page/Page column 25 [25] Journal of the American Chemical Society, 2002, vol. 124, # 41, p. 12182 - 12191 [26] Patent: US5969138, 1999, A [27] Chemical Communications, 2013, vol. 49, # 80, p. 9173 - 9175 [28] Dyes and Pigments, 2013, vol. 99, # 1, p. 185 - 191 [29] European Journal of Medicinal Chemistry, 2014, vol. 84, p. 505 - 515 [30] Patent: CN104250246, 2017, B. Location in patent: Paragraph 0151-0153 [31] Patent: CN107286098, 2017, A. Location in patent: Paragraph 0209-0210
