21543-49-7 2-氯-5-羟甲基吡啶

• [1] Patent: WO2016/154241, 2016, A1. Location in patent: Paragraph 578; 581 [2] Patent: EP1439175, 2004, A1. Location in patent: Page 42-43 [3] Patent: WO2005/56529, 2005, A1. Location in patent: Page/Page column 43

合成路线 3（3. 合成：21543-49-7）

产率：75% 合成条件：With BH 3 In tetrahydrofuran; ethyl acetate 实验步骤：9-氯-5- {3- [2-（6-氯吡啶-3-基）-2-羟乙基氨基]环己基} -3-甲基-5H-异恶唑并[4,3-c]喹啉-4酮向搅拌的6溶液中加入 在N 2气氛下，将氯代烟酸（900mg，5.7mmol）的THF（7mL）溶液加入BH 3（16mL，17.1mmol，1M的THF溶液）中。 将反应混合物搅拌5小时。 将其用甲醇（5mL）淬灭，然后浓缩。 将粗产物溶于EtOAc（30mL）中，用1N NaOH（15mL×3），盐水洗涤，干燥并浓缩。 产量：615mg（75％）的6-氯 - 吡啶-3-基 - 甲醇。 参考文献：

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