主要用于化学合成
化学合成
合成路线 1(1. 合成:1082040-63-8)
产率:84%
合成条件:With iodine; potassium hydroxide In N,N-dimethyl-formamide at 20℃;
实验步骤:1H-吡唑并[3,4-c]吡啶(300mg,2.52mmol,1.00当量),KOH(500mg,8.91mmol,3.50当量)和二碘烷(1.28g,5.04mmol,2.00当量)的悬浮液。 将DMF(10mL)在室温下搅拌过夜。 用水淬灭反应,用乙酸乙酯萃取,用无水硫酸钠干燥,并在真空下浓缩。 通过硅胶柱,用乙酸乙酯/石油醚(1:1)纯化残余物,得到标题化合物(577mg,84%),为黄色固体。 LC-MS(ES,m / z):246 [M + H]。
参考文献:
- [1] Patent: WO2015/25025, 2015, A1. Location in patent: Page/Page column 357 [2] Patent: WO2017/98328, 2017, A2. Location in patent: Paragraph 00222 [3] Patent: WO2018/15818, 2018, A2. Location in patent: Paragraph 00177 [4] Patent: WO2012/93101, 2012, A1. Location in patent: Page/Page column 152 [5] Patent: WO2014/2053, 2014, A1. Location in patent: Page/Page column 51 [6] Patent: WO2014/2051, 2014, A2. Location in patent: Page/Page column 54 [7] Patent: WO2014/2052, 2014, A1. Location in patent: Page/Page column 49 [8] Patent: WO2014/2058, 2014, A2. Location in patent: Page/Page column 60 [9] Patent: WO2014/9833, 2014, A2. Location in patent: Page/Page column 45 [10] Patent: WO2014/2054, 2014, A1. Location in patent: Page/Page column 63