5-氨基-1,3-二氢吲哚-2-酮为酮类衍生物，可用作有机中间体，用于化学合成。
化学合成；有机中间体
路线1：
- 原料：5-硝基-1,3-二氢-吲哚-2-酮（20876-36-2）
- 步骤：将356mg 5-硝基-1,3-二氢-吲哚-2-酮在30ml四氢呋喃：乙醇=1:1混合溶剂中，加入400mg钯/碳（10%）催化剂，在室温和常压下氢化1小时。反应结束后，通过硅藻土吸去催化剂，蒸发浓缩滤液，得到320mg产物。
- 条件：氢气（H₂）；四氢呋喃（THF）与乙醇混合溶剂（1:1）；20℃；常压；1小时
- 产率：100%
- 参考文献：[1] Patent: US2004/39019, 2004, A1. Location in patent: Page/Page column 6；[2] Patent: US6268391, 2001, B1；[3] Journal of Antibiotics, 2018, vol. 71, #10, p. 887-897；[4] European Journal of Medicinal Chemistry, 2015, vol. 105, p. 274-288；[5] Patent: WO2016/198597, 2016, A1. Location in patent: Page/Page column 18; 19；[6] Patent: WO2004/56786, 2004, A2. Location in patent: Page 73；[7] Patent: US2010/75952, 2010, A1. Location in patent: Page/Page column 64；[8] Patent: EP2157093, 2010, A1. Location in patent: Page/Page column 62；[9] Archiv der Pharmazie, 2015, vol. 348, #10, p. 715-729；[10] Patent: US2003/100555, 2003, A1；[11] Patent: US2002/183364, 2002, A1；[12] Patent: US2003/69421, 2003, A1；[13] Patent: US2003/216410, 2003, A1；[14] Patent: US6051593, 2000, A；[15] Patent: US2002/156292, 2002, A1；[16] Patent: US6486185, 2002, B1；[17] Patent: US6114371, 2000, A；[18] Patent: US6147106, 2000, A；[19] Patent: US6846839, 2005, B1；[20] Patent: US6878733, 2005, B1. Location in patent: Page/Page column 168；[21] Patent: US6350754, 2002, B2. Location in patent: Page column 19；[22] Patent: US2005/256145, 2005, A1. Location in patent: Page/Page column 43；[23] Patent: US2005/256144, 2005, A1. Location in patent: Page/Page column 19-20；[24] Patent: US2603659, 1950；[25] Zhurnal Obshchei Khimii, 1956, vol. 26, p. 2019,2023, 2024; engl. Ausg. S. 2251, 2254, 2255；[26] Pharmaceutical Chemistry Journal, 1994, vol. 28, #4, p. 236-242；[27] Khimiko-Farmatsevticheskii Zhurnal, 1994, vol. 28, #4, p. 22-26；[28] Patent: US2005/90541, 2005, A1. Location in patent: Page/Page column 31；[29] Bioorganic and Medicinal Chemistry Letters, 2012, vol. 22, #15, p. 4979-4985；[30] ACS Medicinal Chemistry Letters, 2013, vol. 4, #12, p. 1137-1141；[31] MedChemComm, 2014, vol. 5, #5, p. 655-658；[32] Patent: WO2016/55454, 2016, A1. Location in patent: Page/Page column 10; 11；[33] European Journal of Medicinal Chemistry, 2017, vol. 134, p. 258-270
路线2：
- 原料：5-硝基吲哚（4g，24.6mmol）
- 步骤：向搅拌的5-硝基吲哚在200ml叔丁醇中的溶液中，在0.5小时内分批加入溴化吡啶鎓（30g，93mmol）。反应混合物在室温下搅拌过夜，除去叔丁醇后，将残余物溶于乙酸乙酯/水（500/500ml）中，分离有机层，水层用300ml乙酸乙酯萃取，合并有机萃取液，用水洗涤，无水硫酸钠干燥，真空浓缩，得到8.5g极性较小的化合物，经乙酸乙酯重结晶得到7.5g二溴衍生物。将该二溴衍生物与10当量锌粉在80ml乙酸中于室温下氢化3小时，得到5-氨基羟吲哚。
- 条件：锌粉（Zn）；乙酸；水；乙酸乙酯；叔丁醇；室温；3小时；收率82%
- 参考文献：[1] Patent: US5849710, 1998, A
