化学合成，雷奈佐利中间体，利奈唑胺中间体。
医药
合成路线 1（1. 合成：93246-53-8）
产率：100%
合成条件：With hydrogen In ethanol at 0℃; for 18 h;
实验步骤：描述2：3-氟-4-（4-吗啉基）苯胺4-（2-氟-4-硝基苯基）吗啉D1（42.6g，0.19mol）的乙醇（1.2L）溶液用10％Pd / C糊剂氢化 （4g）在STP持续18h。 将所得混合物通过硅藻土过滤，真空蒸发滤液，得到标题产物（36.9g，100％），为无色固体.1H NMR（CDCl3）8：2.96（4H，m），3.55（2H，br s） ），3.84（4H，m），6.41（2H，m），6.79（1H，m）。
参考文献：
- [1] Patent: WO2005/58317, 2005, A1. Location in patent: Page/Page column 35 [2] Patent: WO2005/58885, 2005, A2. Location in patent: Page/Page column 33 [3] Patent: WO2005/75461, 2005, A1. Location in patent: Page/Page column 100 [4] Patent: WO2006/2956, 2006, A1. Location in patent: Page/Page column 31 [5] Journal of Medicinal Chemistry, 2018, vol. 61, # 9, p. 4052 - 4066 [6] Patent: WO2005/103042, 2005, A1. Location in patent: Page/Page column 32-33 [7] Patent: WO2005/103000, 2005, A1. Location in patent: Page/Page column 33-34 [8] Patent: WO2008/122787, 2008, A1. Location in patent: Page/Page column 70-71 [9] Journal of Chemical Research, 2009, # 12, p. 739 - 740 [10] Journal of Heterocyclic Chemistry, 2012, vol. 49, # 5, p. 1143 - 1146,4 [11] Patent: CN106397358, 2017, A. Location in patent: Paragraph 0039; 0063; 0071; 0081-0083; 0091-0094 [12] ChemMedChem, 2017, vol. 12, # 18, p. 1525 - 1533 [13] Organic Process Research and Development, 2018, vol. 22, # 10, p. 1448 - 1452 [14] Patent: WO2009/32667, 2009, A1. Location in patent: Page/Page column 107 [15] Patent: US2011/275805, 2011, A1. Location in patent: Page/Page column 7 [16] Patent: EP2388251, 2011, A1. Location in patent: Page/Page column 8 [17] Journal of Organic Chemistry, 2013, vol. 78, # 9, p. 4530 - 4542 [18] Letters in Organic Chemistry, 2010, vol. 7, # 1, p. 45 - 49 [19] Patent: WO2011/137222, 2011, A1. Location in patent: Example 5 [20] Patent: CN102617500, 2016, B. Location in patent: Paragraph 0038; 0039 [21] ChemPlusChem, 2018, vol. 83, # 5, p. 375 - 382 [22] Patent: WO2011/114210, 2011, A2. Location in patent: Page/Page column 19 [23] Patent: US2014/24827, 2014, A1. Location in patent: Paragraph 0049-0051 [24] Patent: WO2014/12360, 2014, A1. Location in patent: Paragraph 00272 [25] Patent: US2015/87639, 2015, A1. Location in patent: Paragraph 0519 [26] Patent: TWI607995, 2017, B. Location in patent: Page/Page column 124 [27] Patent: US2011/306606, 2011, A1. Location in patent: Page/Page column 14 [28] Patent: EP2394993, 2011, A2. Location in patent: Page/Page column 21-22 [29] Turkish Journal of Chemistry, 2012, vol. 36, # 1, p. 37 - 53 [30] Patent: WO2009/63505, 2009, A2. Location in patent: Page/Page column 13 [31] J. Med. Chem., 1996, vol. 39, # 3, p. 673 - 679 [32] Bioorganic and Medicinal Chemistry Letters, 2002, vol. 12, # 6, p. 857 - 859 [33] Chemical and Pharmaceutical Bulletin, 2001, vol. 49, # 4, p. 353 - 360 [34] Tetrahedron, 2003, vol. 59, # 19, p. 3403 - 3407 [35] Patent: US2004/87575, 2004, A1 [36] Patent: US2003/13708, 2003, A1 [37] Patent: US2004/110745, 2004, A1 [38] Patent: WO2005/47288, 2005, A1. Location in patent: Page/Page column 48 [39] Synthetic Communications, 2010, vol. 40, # 6, p. 789 - 798 [40] Bioorganic and Medicinal Chemistry Letters, 2010, vol. 20, # 3, p. 1302 - 1305 [41] Patent: WO2011/77310, 2011, A1. Location in patent: Page/Page column 12 [42] Patent: WO2012/114355, 2012, A1. Location in patent: Page/Page column 10 [43] Patent: WO2013/72923, 2013, A1. Location in patent: Page/Page column 15-16 [44] European Journal of Medicinal Chemistry, 2013, vol. 69, p. 779 - 785 [45] Patent: US2013/324719, 2013, A1. Location in patent: Paragraph 0022; 0046-0047 [46] Bioorganic and Medicinal Chemistry Letters, 2015, vol. 25, # 4, p. 874 - 880 [47] European Journal of Organic Chemistry, 2014, vol. 2014, # 34, p. 7614 - 7620 [48] European Journal of Medicinal Chemistry, 2015, vol. 106, p. 120 - 131 [49] Patent: WO2015/162622, 2015, A1. Location in patent: Page/Page column 9; 10 [50] Patent: CN103420933, 2016, B. Location in patent: Paragraph 0032; 0056-0057
