76360-82-2 2-(甲硫基)-4-(甲氨基)嘧啶-5-甲酸乙酯

运输信息：冰袋运输。危险描述：非危险化学品。

作为医药中间体或潜在药物分子，用于相关药物研发与合成。

医药

路线1：

• 步骤: 在0℃下，将EtOH中的甲胺（33％，17.5mL，140mmol）缓慢加入到中间体3（10.0g，43.1mmol）在120mL二氯甲烷中的溶液中；搅拌30分钟；加入水（150ml），分离混合物，干燥有机层，过滤，浓缩得到标题化合物。
• 条件: 0℃；反应时间0.50小时；溶剂为二氯甲烷、乙醇、水。
• 收率: 100%。
• 参考文献: [1] Patent: WO2014/144737, 2014, A1. Location in patent: Paragraph 00719 [2] Patent: WO2015/19037, 2015, A1. Location in patent: Page/Page column 87; 88 [3] Patent: US2003/207900, 2003, A1. Location in patent: Page/Page column 15 [4] Journal of Medicinal Chemistry, 2010, vol. 53, # 15, p. 5439 - 5448 [5] Journal of Medicinal Chemistry, 2011, vol. 54, # 7, p. 2255 - 2265 [6] Patent: WO2014/11900, 2014, A2. Location in patent: Page/Page column 30; 31 [7] Patent: US2015/197519, 2015, A1. Location in patent: Paragraph 0166; 0167 [8] Patent: US9695165, 2017, B2. Location in patent: Page/Page column 48 [9] Patent: WO2016/168992, 2016, A1. Location in patent: Paragraph 151 [10] Patent: US2014/323464, 2014, A1. Location in patent: Paragraph 0466-0468 [11] Patent: WO2004/63195, 2004, A1. Location in patent: Page 53 [12] Patent: WO2015/6492, 2015, A1. Location in patent: Page/Page column 85 [13] Patent: WO2006/71940, 2006, A2. Location in patent: Page/Page column 354 [14] Patent: WO2008/33999, 2008, A2. Location in patent: Page/Page column 87-88 [15] Bioorganic and Medicinal Chemistry, 2005, vol. 13, # 16, p. 4936 - 4951 [16] Journal of Medicinal Chemistry, 1998, vol. 41, # 17, p. 3276 - 3292 [17] Journal of Medicinal Chemistry, 2014, vol. 57, # 3, p. 578 - 599 [18] Patent: WO2006/82492, 2006, A1. Location in patent: Page/Page column 33-34 [19] Patent: WO2008/55842, 2008, A1. Location in patent: Page/Page column 41-42 [20] Patent: US2009/36472, 2009, A1. Location in patent: Page/Page column 22 [21] Patent: WO2004/14907, 2004, A1. Location in patent: Page 29-30 [22] ACS Medicinal Chemistry Letters, 2015, vol. 6, # 4, p. 413 - 418 [23] Bioorganic and Medicinal Chemistry Letters, 2016, vol. 26, # 9, p. 2138 - 2141 [24] Patent: WO2008/78249, 2008, A1. Location in patent: Page/Page column 22

路线2：

• 步骤: 20g（86mmol）4-氯-2-甲硫基嘧啶-5-羧酸乙酯的溶液（Aldrich Chemical Co.，Milwaukee，Wis。，USA）在250mL二氯甲烷中冷却至0℃，用35mL（281mmol）33％甲胺的乙醇溶液缓慢处理；搅拌30分钟后，加入150mL水，分离各相；有机相用硫酸镁干燥并过滤；减压蒸发滤液得到产物。
• 条件: 0℃；溶剂为二氯甲烷、乙醇、水；反应时间30分钟。
• 收率: 97%。
• 参考文献: [1] Patent: US2003/171584, 2003, A1 [2] Patent: US2002/55513, 2002, A1 [3] Patent: US6451804, 2002, B1 [4] Patent: US6498163, 2002, B1 [5] Patent: US6150373, 2000, A [6] Patent: US2004/224958, 2004, A1