- 4-氟苯甲酰肼是一种有机中间体，可作为有机合成中间体和医药中间体，主要用于实验室研发过程和化工生产过程中。
- 制备
在250mL的三口瓶中加入对氟苯甲酸(10.0g，60mmol)和100mL四氢呋喃，再加入N,N'-羰基二咪唑(12.6g，78mmol)，TLC监测原料反应是否完全，反应完毕后，缓慢滴加80％水合肼(5.94g，95mmol)，滴毕，搅拌反应6小时左右。
TLC监测原料反应是否完全(展开剂：石油醚/乙酸乙酯1:1)。反应完毕后，冷至
室温，减压浓缩除去大部分有机溶剂，加水约30mL，室温下打浆片刻，抽滤，水洗，得白色片状固体。经15mL无水乙醇重结晶得4-氟苯甲酰肼，白色固体6.91g，收
率75.2％。
有机合成中间体; 医药中间体
合成路线 1（1. 合成：456-06-4）
产率：100%
合成条件：With hydrazine hydrate In ethanol at 20 - 85℃; for 10 h; Reflux
实验步骤：在室温下向搅拌的4-氟乙基苯甲酸酯（4.5g，26.7mmol）的EtOH（30mL）溶液中加入NH 2 NH 2 .H 2 O（6.67g，133.5mmol），并将溶液在85℃下回流10小时。 将反应冷却至室温，减压浓缩，用正己烷（50mL）洗涤固体，然后干燥，得到4-氟苯甲酰肼固体（4.2g，定量收率）。 1H NMR（400MHz，DMSO-d6）：δ9.85（s，1H），7.86（dd，2H），7.25（t，3H），4.46（s，1H），3.47（br s，1H）。
参考文献：
- [1] Patent: WO2013/49559, 2013, A1. Location in patent: Page/Page column 92 [2] Bioorganic and Medicinal Chemistry, 2015, vol. 23, # 17, p. 6014 - 6024 [3] Patent: WO2011/52516, 2011, A1. Location in patent: Page/Page column 59 [4] Journal of Nanoscience and Nanotechnology, 2013, vol. 13, # 5, p. 3321 - 3330 [5] European Journal of Medicinal Chemistry, 2010, vol. 45, # 9, p. 3943 - 3949 [6] European Journal of Medicinal Chemistry, 2010, vol. 45, # 9, p. 3960 - 3969 [7] Journal of Labelled Compounds and Radiopharmaceuticals, 2006, vol. 49, # 2, p. 125 - 137 [8] Patent: JP5787538, 2015, B2. Location in patent: Paragraph 0161; 0162 [9] Journal of the American Chemical Society, 1950, vol. 72, p. 1806 [10] Journal of Medicinal Chemistry, 2003, vol. 46, # 16, p. 3463 - 3475 [11] Journal of Agricultural and Food Chemistry, 2003, vol. 51, # 1, p. 152 - 155 [12] Bioorganic and Medicinal Chemistry Letters, 2006, vol. 16, # 8, p. 2278 - 2282 [13] Tetrahedron, 2008, vol. 64, # 8, p. 1860 - 1867 [14] European Journal of Medicinal Chemistry, 2009, vol. 44, # 5, p. 2113 - 2121 [15] European Journal of Medicinal Chemistry, 2009, vol. 44, # 9, p. 3798 - 3804 [16] Journal of Medicinal Chemistry, 2009, vol. 52, # 14, p. 4200 - 4209 [17] Journal of Chemical Research, 2010, # 7, p. 410 - 413 [18] Journal of Medicinal Chemistry, 2010, vol. 53, # 20, p. 7392 - 7404 [19] Bioorganic and Medicinal Chemistry, 2010, vol. 18, # 22, p. 7836 - 7841 [20] Bioorganic and Medicinal Chemistry Letters, 2009, vol. 19, # 2, p. 332 - 335 [21] Journal of Chemical Research, 2010, vol. 34, # 12, p. 680 - 683 [22] Journal of Chemical Research, 2011, vol. 35, # 4, p. 234 - 237 [23] Journal of Chemical Research, 2011, vol. 35, # 6, p. 364 - 367 [24] Medicinal Chemistry Research, 2012, vol. 21, # 11, p. 3646 - 3655 [25] Organic Preparations and Procedures International, 2017, vol. 49, # 4, p. 370 - 376 [26] Bioorganic and Medicinal Chemistry, 2013, vol. 21, # 8, p. 2286 - 2297 [27] Bioorganic and Medicinal Chemistry Letters, 2014, vol. 24, # 22, p. 5154 - 5156 [28] Journal of the Chemical Society of Pakistan, 2013, vol. 35, # 3, p. 929 - 937 [29] Medicinal Chemistry Research, 2013, vol. 22, # 11, p. 5344 - 5348 [30] Journal of Chemical Research, 2014, vol. 38, # 5, p. 300 - 303 [31] Bioorganic and Medicinal Chemistry Letters, 2015, vol. 25, # 15, p. 3052 - 3056 [32] Journal of Heterocyclic Chemistry, 2015, vol. 52, # 5, p. 1296 - 1301 [33] Journal of Heterocyclic Chemistry, 2017, vol. 54, # 2, p. 1423 - 1429 [34] Asian Journal of Chemistry, 2015, vol. 27, # 10, p. 3605 - 3608 [35] Asian Journal of Chemistry, 2016, vol. 28, # 3, p. 639 - 643 [36] Bioorganic Chemistry, 2016, vol. 65, p. 126 - 136 [37] Bioorganic and Medicinal Chemistry, 2016, vol. 24, # 8, p. 1879 - 1888 [38] Patent: WO2016/108249, 2016, A1. Location in patent: Paragraph 053 [39] Journal of the Brazilian Chemical Society, 2016, vol. 27, # 11, p. 1998 - 2010 [40] Chemical Biology and Drug Design, 2017, vol. 90, # 2, p. 236 - 243 [41] Bioorganic and Medicinal Chemistry, 2017, vol. 25, # 20, p. 5652 - 5661 [42] Chinese Journal of Chemistry, 2017, vol. 35, # 9, p. 1437 - 144 [43] Oriental Journal of Chemistry, 2017, vol. 33, # 6, p. 2930 - 2936 [44] RSC Advances, 2018, vol. 8, # 12, p. 6306 - 6314 [45] Patent: CN108218848, 2018, A. Location in patent: Paragraph 0152; 0153; 0155 [46] Patent: CN104892639, 2018, B. Location in patent: Paragraph 0065
