54840-15-2 4-(Boc-氨基)酚

常温运输。WGK Germany:3。危险等级:IRRITANT。存储类别:11 - 可燃固体。危险性类别:眼部刺激 类别2；经皮刺激 类别2；特异性靶器官毒性-一次接触，类别3。非危险化学品。

化学合成。

化学合成

合成路线 1（1. 合成：54840-15-2）

产率：100% 合成条件：With triethylamine In methanol at 22℃; for 14 h; 实验步骤：向4-氨基苯酚（10.97g，100.5mmol）和三乙胺（30mL）的甲醇（200mL）溶液中加入二碳酸二叔丁酯（24.07g，110.3mmol）。将反应混合物在22℃下搅拌14小时。除去溶剂后，将残余物在乙酸乙酯（250mL）和0.25N盐酸水溶液（100mL）之间分配。分离有机相，用饱和氯化铵水溶液（3×50mL）洗涤，并用无水硫酸钠干燥。除去溶剂，得到白色固体（20.91g，100％收率，ES-（m / z）208.1 [M-H]）。 参考文献：[1] Patent: EP1609789, 2005, A1. Location in patent: Page/Page column 12 [2] Tetrahedron Letters, 2011, vol. 52, # 12, p. 1260 - 1264 [3] Chemical Communications, 2013, vol. 49, # 51, p. 5757 - 5759 [4] Organic Letters, 2016, vol. 18, # 21, p. 5728 - 5731 [5] Comptes Rendus Chimie, 2013, vol. 16, # 11, p. 962 - 966 [6] Tetrahedron Letters, 2006, vol. 47, # 46, p. 8039 - 8042 [7] Patent: US2012/65384, 2012, A1. Location in patent: Page/Page column 13 [8] Journal of Molecular Catalysis A: Chemical, 2013, vol. 370, p. 111 - 116 [9] RSC Advances, 2013, vol. 3, # 32, p. 13324 - 13328 [10] Journal of Chemical Research, 2013, vol. 37, # 12, p. 757 - 760 [11] Research on Chemical Intermediates, 2016, vol. 42, # 2, p. 1451 - 1461 [12] Research on Chemical Intermediates, 2017, vol. 43, # 3, p. 1355 - 1363 [13] Photochemical and Photobiological Sciences, 2017, vol. 16, # 8, p. 1260 - 1267 [14] Journal of Medicinal Chemistry, 2005, vol. 48, # 19, p. 5989 - 6003 [15] Patent: WO2009/36016, 2009, A1. Location in patent: Page/Page column 80 [16] Bioorganic and Medicinal Chemistry Letters, 2013, vol. 23, # 7, p. 2217 - 2219 [17] RSC Advances, 2016, vol. 6, # 82, p. 78576 - 78584 [18] Organic Letters, 2017, vol. 19, # 18, p. 4972 - 4975 [19] Patent: CN107400072, 2017, A. Location in patent: Paragraph 0035; 0108; 0109 [20] European Journal of Organic Chemistry, 2018, vol. 2018, # 6, p. 829 - 836 [21] New Journal of Chemistry, 2018, vol. 42, # 12, p. 10142 - 10147 [22] New Journal of Chemistry, 2018, vol. 42, # 14, p. 12152 - 12161 [23] Organic and Biomolecular Chemistry, 2006, vol. 4, # 14, p. 2769 - 2771 [24] Tetrahedron Letters, 2007, vol. 48, # 47, p. 8318 - 8322 [25] Chemistry Letters, 2010, vol. 39, # 11, p. 1127 - 1129 [26] ACS Medicinal Chemistry Letters, 2015, vol. 6, # 10, p. 1059 - 1064 [27] Journal of Medicinal Chemistry, 1995, vol. 38, # 20, p. 3983 - 3994 [28] Journal of Medicinal Chemistry, 2013, vol. 56, # 24, p. 9982 - 10002 [29] European Journal of Organic Chemistry, 2009, # 25, p. 4290 - 4299 [30] Comptes Rendus Chimie, 2014, vol. 17, # 2, p. 164 - 170 [31] RSC Advances, 2014, vol. 4, # 47, p. 24544 - 24550 [32] Organic and Biomolecular Chemistry, 2018, vol. 16, # 12, p. 2143 - 2149 [33] Patent: EP2636669, 2013, A1. Location in patent: Paragraph 0141; 0142 [34] Letters in Organic Chemistry, 2013, vol. 10, # 2, p. 121 - 125 [35] Patent: US2013/225585, 2013, A1. Location in patent: Paragraph 0229; 0230; 0231 [36] Journal of the Chinese Chemical Society, 2011, vol. 58, # 4, p. 538 - 543 [37] Chinese Journal of Catalysis, 2013, vol. 34, # 9, p. 1730 - 1733 [38] Tetrahedron Letters, 2008, vol. 49, # 16, p. 2527 - 2532 [39] Chemical Communications, 2017, vol. 53, # 58, p. 8188 - 8191 [40] Organic Letters, 2006, vol. 8, # 15, p. 3259 - 3262 [41] Tetrahedron Letters, 2006, vol. 47, # 7, p. 1087 - 1091 [42] Journal of the American Chemical Society, 2018, vol. 140, # 44, p. 15114 - 15123 [43] Patent: WO2014/118133, 2014, A1. Location in patent: Page/Page column 25 [44] Journal of Medicinal Chemistry, 2017, vol. 60, # 14, p. 6384 - 6399 [45] Patent: US2010/48570, 2010, A1. Location in patent: Page/Page column 49 [46] Journal of Medicinal Chemistry, 2014, vol. 57, # 10, p. 4239 - 4251 [47] Monatshefte fur Chemie, 2017, vol. 148, # 6, p. 1069 - 1074 [48] Journal of Organic Chemistry, 2011, vol. 76, # 17, p. 7132 - 7140 [49] Patent: WO2005/48948, 2005, A2. Location in patent: Page/Page column 167 [50] Patent: WO2005/48948, 2005, A2. Location in patent: Page/Page column 167 [51] Tetrahedron, 1994, vol. 50, # 19, p. 5621 - 5632 [52] European Journal of Organic Chemistry, 1999, # 6, p. 1357 - 1366 [53] Bioorganic and Medicinal Chemistry Letters, 2003, vol. 13, # 24, p. 4293 - 4297 [54] Bioorganic and Medicinal Chemistry Letters, 2006, vol. 16, # 7, p. 2017 - 2021 [55] Bioorganic and Medicinal Chemistry, 2006, vol. 14, # 19, p. 6525 - 6538 [56] Chemistry Letters, 2007, vol. 36, # 5, p. 682 - 683 [57] Bioorganic and Medicinal Chemistry Letters, 2007, vol. 17, # 19, p. 5349 - 5352 [58] Patent: US4987132, 1991, A [59] Tetrahedron, 2009, vol. 65, # 8, p. 1618 - 1629 [60] Patent: US6388022, 2002, B1. Location in patent: Page column 26 [61] Patent: WO2005/47288, 2005, A1. Location in patent: Page/Page column 49-50 [62] Journal of the Chinese Chemical Society (Taipei, Taiwan), 2009, vol. 56, # 1, p. 121 - 126 [63] Journal of the American Chemical Society, 2010, vol. 132, # 5, p. 1523 - 1525 [64] Patent: WO2006/44707, 2006, A1. Location in patent: Page/Page column 53-54 [65] Bioconjugate Chemistry, 2010, vol. 21, # 11, p. 2110 - 2118 [66] Tetrahedron, 2011, vol. 67, # 45, p. 8731 - 8739 [67] European Journal of Medicinal Chemistry, 2013, vol. 62, p. 728 - 737 [68] Monatshefte fur Chemie, 2014, vol. 145, # 3, p. 509 - 515 [69] Patent: US2015/183777, 2015, A1. Location in patent: Paragraph 0172; 0173 [70] Patent: WO2017/158612, 2017, A1. Location in patent: Page/Page column 26