1H-吡唑基[3,4-B]吡啶-3-羧酸为羧酸类衍生物,可用作医药合成中间体,用于医药合成和医药实验研究;制备方法:室温下,在三口烧瓶中加入2-氯-3-乙酰基吡啶,以水合肼为溶剂,有机溶剂中搅拌反应1小时,升温回流过夜,冷却后萃取、干燥、层析纯化得到产物。
医药
路线1:
- 步骤:向NaOH水溶液中加入3-甲基-1H-吡唑并[3,4-p]吡啶,加热至澄清;缓慢加入KMnO₄水溶液,80℃反应2小时后90℃继续2小时;冷却至70℃过滤,沸水洗涤,滤液冷却至0℃,酸化后正丁醇萃取,减压浓缩、溶解过滤得产物。
- 条件:80-90℃;
- 产率:81%;
- 参考文献:[1] Patent: WO2011/84486, 2011, A1. Location in patent: Page/Page column 106; 111-112 [2] Patent: US2013/296302, 2013, A1. Location in patent: Paragraph 0496 [3] Patent: US2016/68550, 2016, A1. Location in patent: Paragraph 1058 [4] Patent: WO2016/40193, 2016, A1. Location in patent: Paragraph 0705 [5] Canadian Journal of Chemistry, 1988, vol. 66, # 3, p. 420-428 [6] Patent: US2006/47126, 2006, A1. Location in patent: Page/Page column 30-31 [7] Patent: WO2011/5759, 2011, A2. Location in patent: Page/Page column 78