4093-28-1 4-乙酰氨基-2-羟基苯甲酸甲酯

常温运输。危险等级为IRRITANT（刺激性），海关编码2916399090，非危险化学品。

化学合成，医药胃复安的中间体；医药、化工中间体。

医药; 化工

路线1：

• 步骤: 将4-氨基-2-羟基苯甲酸甲酯在乙酸乙酯中的溶液加入水和碳酸氢钠溶液，冷却后加入乙酰氯，逐渐温热至室温并搅拌，分离有机层，洗涤、干燥、减压除溶剂得产品。
• 条件: With sodium hydrogencarbonate In water; ethyl acetate at 0 - 20℃; for 2.25 h
• 收率: 99%
• 参考文献: [1] Patent: WO2013/42135, 2013, A1. Location in patent: Page/Page column 11 [2] Patent: US2014/187581, 2014, A1. Location in patent: Paragraph 0095-0097 [3] Organic Process Research and Development, 2010, vol. 14, # 1, p. 92 - 98 [4] Patent: US2016/251376, 2016, A1. Location in patent: Paragraph 0955; 0956; 0957 [5] Bioorganic and Medicinal Chemistry Letters, 1996, vol. 6, # 22, p. 2657 - 2662 [6] Chemical and Pharmaceutical Bulletin, 1997, vol. 45, # 12, p. 2079 - 2084 [7] Patent: US4857517, 1989, A [8] Patent: US4859683, 1989, A

路线2：

• 步骤: 向三颈烧瓶中加入4-氨基-2-羟基苯甲酸甲酯和冰醋酸，升温至40℃，加入乙酸酐，反应完成后加水，冷却抽滤，洗涤干燥得产品。
• 条件: at 40℃; for 1 h
• 收率: 92.4%
• 参考文献: [1] Tetrahedron, 1986, vol. 42, # 12, p. 3259 - 3268 [2] Chemistry - An Asian Journal, 2016, vol. 11, # 9, p. 1376 - 1381 [3] Patent: CN107337658, 2017, A. Location in patent: Paragraph 0041; 0042 [4] Patent: US2012/101157, 2012, A1. Location in patent: Page/Page column 9 [5] Bioorganic and Medicinal Chemistry, 2008, vol. 16, # 7, p. 3839 - 3847 [6] Patent: WO2007/48643, 2007, A1. Location in patent: Page/Page column 12; 27-28 [7] Patent: WO2016/128990, 2016, A1. Location in patent: Page/Page column 25-26 [8] Journal of the Chemical Society, 1949, p. 1498,1502 [9] Letters in Drug Design and Discovery, 2012, vol. 9, # 5, p. 489 - 493

路线3：

• 步骤: 将乙酸钠三水合物加入对氨基水杨酸甲酯反应溶液，控制pH 6.5-7.5，温度35-40℃，加入乙酰酶反应2小时，减压回收甲醇，萃取、分液、干燥、浓缩、结晶、抽滤、干燥得产品。
• 条件: at 35 - 40℃; for 2 h; Enzymatic reaction
• 收率: 95.2%
• 参考文献: [1] Patent: CN107540568, 2018, A. Location in patent: Paragraph 0022; 0024