1000802-52-7
1000802-52-7 结构式
基本信息
1-(2-(pyrrolidin-1-yl)ethyl)-4-(4,4,5,5-tetramethyl-1,3,2-di...
1-[2-(pyrrolidin-1-yl)ethyl]-4-(tetraMethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
1-[2-(1-Pyrrolidinyl)ethyl]-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
1-(2-(pyrrolidin-1-yl)ethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
1H-Pyrazole, 1-[2-(1-pyrrolidinyl)ethyl]-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-
物理化学性质
制备方法
269410-08-4
7250-67-1
1000802-52-7
以4-吡唑硼酸频哪醇酯（1.7g，8.8mmol）和N-(2-氯乙基)吡咯烷盐酸盐（1.48g，8.70mmol）为原料，在碳酸钾（3.7g，27.00mmol）存在下，于DMF（15mL）中80℃搅拌反应6小时。反应完成后，将反应混合物用水（50mL）稀释，并用二氯甲烷（50mL×3）萃取。合并有机层，用饱和氯化钠水溶液（15mL）洗涤，无水硫酸钠干燥，减压浓缩。通过硅胶柱色谱法纯化残余物，以二氯甲烷/乙酸乙酯（v/v，20/1）为洗脱剂，得到浅黄色液体产物1-[2-(1-吡咯烷)乙基]-4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)-1H-吡唑（1.27g，收率50.10%）。质谱（ESI，正离子模式）m/z：292.10 [M + 1]+。
参考文献：
[1] Patent: WO2016/615, 2016, A1. Location in patent: Paragraph 00719
[2] Patent: US2010/273796, 2010, A1. Location in patent: Page/Page column 20-21
[3] Patent: US2011/34474, 2011, A1. Location in patent: Page/Page column 22
[4] Patent: US2011/71153, 2011, A1. Location in patent: Page/Page column 21
[5] Patent: US2011/92498, 2011, A1. Location in patent: Page/Page column 20-21