78981-25-6 N-Boc-D-丙氨酰胺

N-Boc-D-丙氨酰胺主要作为医药中间体，用于相关药物合成研究。

医药

合成路线 1（1. 合成：78981-25-6）

产率：89% 合成条件：Stage #1: With chloroformic acid ethyl ester; triethylamine In tetrahydrofuran at -10℃; for 1 h; Inert atmosphere Stage #2: With ammonia In tetrahydrofuran at -10 - 20℃; Inert atmosphere 实验步骤：通用方法：在-10℃下向搅拌的N-Boc-（R） - 丙氨酸（5.0g，26.4mmol）的无水THF溶液中加入三乙胺（3mL，21.12mmol）和氯甲酸乙酯（2.5mL， 26.4mmol）。 将反应混合物搅拌1小时，然后鼓入NH 3（g）1.5小时。 然后将混合物在室温下搅拌过夜。 然后，在减压下除去THF，之后加入NaCl。溶胶。 加入（40mL）并用EtOAc（5×40mL）萃取。 用0.5M HCl（2×30mL）洗涤有机层，用Na 2 SO 4干燥，过滤，真空蒸发，得到酰胺。 参考文献：

• [1] Tetrahedron, 1999, vol. 55, # 42, p. 12301 - 12308 [2] Tetrahedron Letters, 2007, vol. 48, # 4, p. 603 - 607 [3] Synthetic Communications, 2013, vol. 43, # 7, p. 993 - 1006 [4] Bulletin of the Chemical Society of Japan, 1988, vol. 61, # 7, p. 2647 - 2648 [5] Tetrahedron Asymmetry, 2013, vol. 24, # 24, p. 1572 - 1575 [6] Tetrahedron Letters, 1995, vol. 36, # 39, p. 7115 - 7118 [7] Angewandte Chemie - International Edition, 2008, vol. 47, # 23, p. 4331 - 4334 [8] Patent: US2011/212967, 2011, A1. Location in patent: Page/Page column 11 [9] Inorganic Chemistry, 2016, vol. 55, # 2, p. 877 - 886 [10] Patent: US2005/131042, 2005, A1. Location in patent: Page/Page column 124 [11] Patent: US2011/3827, 2011, A1. Location in patent: Page/Page column 111-112 [12] Tetrahedron Letters, 2007, vol. 48, # 8, p. 1465 - 1468 [13] Chemical Communications, 2006, # 4, p. 460 - 462 [14] Synthetic Communications, 2009, vol. 39, # 3, p. 395 - 406 [15] Bioorganic and Medicinal Chemistry Letters, 2009, vol. 19, # 16, p. 4878 - 4881 [16] Journal of Organic Chemistry, 2011, vol. 76, # 23, p. 9845 - 9851 [17] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 24, p. 7355 - 7358 [18] Organic Letters, 2012, vol. 14, # 5, p. 1198 - 1201 [19] Organic Letters, 2013, vol. 15, # 18, p. 4638 - 4641 [20] European Journal of Organic Chemistry, 2013, # 36, p. 8154 - 8161 [21] Tetrahedron Letters, 2014, vol. 55, # 15, p. 2389 - 2393 [22] Tetrahedron Letters, 2014, vol. 55, # 50, p. 6831 - 6835 [23] MedChemComm, 2015, vol. 6, # 2, p. 300 - 305 [24] Patent: WO2016/142833, 2016, A1. Location in patent: Page/Page column 69 [25] ACS Medicinal Chemistry Letters, 2017, vol. 8, # 4, p. 401 - 406 [26] Patent: WO2009/146112, 2009, A1. Location in patent: Page/Page column 29; 33