化学合成；生命科学。
医药
合成路线 1（1. 合成：41088-86-2）
产率：8.55 g
合成条件：With sodium carbonate In 1,4-dioxane; water at 20℃; Cooling with ice
实验步骤：将L-高丝氨酸（4.76g，40mmol）和Na 2 CO 3（8.48g，80mmol）溶于水（200mL）中。向该溶液中加入1,4-二恶烷（50mL）并搅拌5分钟。 在冰浴下将Boc 2 O（13.80mL，60mmol）加入到该溶液中并在室温下搅拌过夜。 用石油醚洗涤混合物。 加入另外的水并用HCl（2mol / L）将pH酸化至2以形成沉淀物。 将悬浮液用EtOAc萃取，将合并的有机层用水和盐水洗涤; 用无水Na 2 SO 4干燥; 过滤并浓缩（残留物~8.55g）。
参考文献：
- [1] Journal of Organic Chemistry, 1986, vol. 51, # 26, p. 5047 - 5050 [2] Journal of Peptide Science, 2013, vol. 19, # 5, p. 308 - 314 [3] Journal of Organic Chemistry, 2008, vol. 73, # 8, p. 3212 - 3217 [4] Tetrahedron Letters, 2002, vol. 43, # 33, p. 5727 - 5729 [5] Journal of Organic Chemistry, 2003, vol. 68, # 23, p. 8853 - 8858 [6] Synthesis, 2005, # 6, p. 888 - 892 [7] Patent: US5122523, 1992, A [8] Journal of Medicinal Chemistry, 2009, vol. 52, # 15, p. 4650 - 4656 [9] Journal of Medicinal Chemistry, 2010, vol. 53, # 18, p. 6720 - 6729 [10] Patent: EP2520565, 2012, A1. Location in patent: Page/Page column 10 [11] Patent: WO2014/127052, 2014, A1. Location in patent: Page/Page column 14 [12] Journal of the American Chemical Society, 2015, vol. 137, # 12, p. 4078 - 4081 [13] Biochemistry, 2017, vol. 56, # 8, p. 1062 - 1074 [14] Bioorganic and Medicinal Chemistry, 2017, vol. 25, # 9, p. 2617 - 2624 [15] Tetrahedron Letters, 2017, vol. 58, # 42, p. 3970 - 3973 [16] Patent: WO2017/156074, 2017, A1. Location in patent: Paragraph 00493 [17] Patent: WO2017/189866, 2017, A1. Location in patent: Paragraph 0242 [18] Patent: CN107586265, 2018, A. Location in patent: Paragraph 0083-0086
