175854-39-4 1,4,7-三叔丁氧羰基-1,4,7,10-四氮杂环十二烷

WGK Germany:3 海关编码:29339900 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

概述 1,4,7-三叔丁氧羰基-1,4,7,10-四氮杂环十二烷 是一种双功能螯合剂。双功能螯合剂可用于将放射性金属稳定地连接到放射性药物的载体部。

医药

合成路线 1（1. 合成：175854-39-4）

产率：80% 合成条件：With triethylamine In chloroform at 20℃; 实验步骤：通过加料漏斗将二碳酸二叔丁酯（1.77g，8.12mmol）的氯仿（10mL）溶液缓慢加入到cyclen（7,0.51g，2.90mmol）和三乙胺（1.25mL，8.99mmol）的溶液中。 在室温下在氯仿（40mL）中。 将反应混合物在室温搅拌过夜，然后通过旋转蒸发浓缩。 所得残余物通过硅胶柱色谱纯化，用乙酸乙酯至5％甲醇/二氯甲烷梯度洗脱，得到产物，为白色固体（1.02g，80％）。 表征与之前的报告相符.61 参考文献：

• [1] Journal of Materials Chemistry, 2012, vol. 22, # 36, p. 18784 - 18787 [2] Journal of the American Chemical Society, 2004, vol. 126, # 30, p. 9248 - 9256 [3] RSC Advances, 2016, vol. 6, # 28, p. 23645 - 23652 [4] Journal of Organic Chemistry, 2005, vol. 70, # 1, p. 115 - 123 [5] Chemical Communications, 2011, vol. 47, # 21, p. 6036 - 6038 [6] Tetrahedron, 2011, vol. 67, # 21, p. 3803 - 3808 [7] Angewandte Chemie - International Edition, 2006, vol. 45, # 32, p. 5340 - 5344 [8] Inorganica Chimica Acta, 2011, vol. 365, # 1, p. 38 - 48 [9] Journal of the American Chemical Society, 2011, vol. 133, # 51, p. 20704 - 20707 [10] Research on Chemical Intermediates, 2012, vol. 38, # 8, p. 2085 - 2096 [11] Angewandte Chemie - International Edition, 2006, vol. 45, # 17, p. 2745 - 2748 [12] Tetrahedron, 2006, vol. 62, # 24, p. 5748 - 5755 [13] Inorganic Chemistry, 2017, vol. 56, # 7, p. 3773 - 3780 [14] Journal of the American Chemical Society, 1997, vol. 119, # 13, p. 3068 - 3076 [15] Patent: US2008/193384, 2008, A1. Location in patent: Page/Page column 4-5 [16] Patent: WO2014/153624, 2014, A1. Location in patent: Page/Page column 42; 43 [17] Bulletin de la Societe Chimique de France, 1996, vol. 133, # 1, p. 65 - 73 [18] Chemistry - A European Journal, 2010, vol. 16, # 17, p. 5018 - 5025 [19] Advanced Synthesis and Catalysis, 2014, vol. 356, # 6, p. 1243 - 1254 [20] Patent: CN108047209, 2018, A. Location in patent: Paragraph 0041; 0051; 0052 [21] Patent: WO2015/179955, 2015, A1. Location in patent: Paragraph 00107; 00108; 00109 [22] Bioorganic and Medicinal Chemistry Letters, 2016, vol. 26, # 18, p. 4542 - 4547 [23] Patent: WO2009/10580, 2009, A1. Location in patent: Page/Page column 23; 30-31 [24] Patent: WO2010/84090, 2010, A1. Location in patent: Page/Page column 43; 44 [25] Angewandte Chemie - International Edition, 2018, vol. 57, # 6, p. 1611 - 1615 [26] Angew. Chem., 2018, vol. 130, # 6, p. 1627 - 1631,5 [27] Patent: JP2018/135304, 2018, A. Location in patent: Paragraph 0041; 0042 [28] Synlett, 2004, # 3, p. 453 - 456 [29] Journal of Organic Chemistry, 2007, vol. 72, # 2, p. 376 - 385 [30] Bioorganic and Medicinal Chemistry, 2007, vol. 15, # 2, p. 696 - 701 [31] Bioorganic Chemistry, 2005, vol. 33, # 5, p. 374 - 385 [32] Chemistry and Biodiversity, 2009, vol. 6, # 8, p. 1273 - 1282 [33] Chemistry - A European Journal, 2010, vol. 16, # 43, p. 12935 - 12940 [34] Inorganica Chimica Acta, 2010, vol. 363, # 12, p. 2896 - 2904 [35] Frontiers of Chemistry in China, 2010, vol. 5, # 2, p. 184 - 192 [36] Journal of Coordination Chemistry, 2015, vol. 68, # 2, p. 335 - 349 [37] Patent: CN104478984, 2016, B. Location in patent: Paragraph 0061-0063