870238-67-8

基本信息
4-氰基-3-氟苯硼酸頻哪醇酯
3-氟-4-氰基苯硼酸頻吶醇酯
4-氰基-3-氟苯基硼酸頻鈉醇
4-氰基-3-氟苯基硼酸頻哪醇酯
4-氰基-3-氟苯硼酸頻哪醇酯,96%
2-氟-4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)苯甲腈
4-Cyano-3-fluorophenylboronic acid pinacol ester
2-Fluoro-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborola
4-Cyano-3-fluorobenzeneboronicacidpinacolester,96%
4-Cyano-3-fluorobenzeneboronic acid pinacol ester, 96%
2-(4-Cyano-3-fluorophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
2-Fluoro-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)benzonitrile
BENZONITRILE,2-FLUORO-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-
物理化學(xué)性質(zhì)
制備方法

105942-08-3

73183-34-3

870238-67-8
在氮氣保護下,將4-溴-2-氟苯腈(4.0 g,20 mmol)、聯(lián)硼酸頻那醇酯(3.8 g,30 mmol)和乙酸鉀(6.1 g,60 mmol)懸浮于二甲基亞砜(DMSO,50 mL)中。隨后加入[1,1'-雙(二苯基膦)二茂鐵]二氯化鈀(Pd(dppf)Cl2,1.5 g,0.2 mmol)。將反應(yīng)混合物在80℃下攪拌反應(yīng)4小時。反應(yīng)完成后,將混合物用水(100 mL)稀釋,并用乙酸乙酯(100 mL × 3)進行萃取。合并有機層,依次用水(50 mL × 3)和飽和食鹽水(50 mL)洗滌,然后用無水硫酸鈉干燥。干燥后過濾,濾液經(jīng)減壓濃縮。殘余物通過硅膠柱色譜法(洗脫劑比例:石油醚/乙酸乙酯 = 50:1至10:1)純化,得到目標(biāo)產(chǎn)物4-氰基-3-氟苯基硼酸頻哪醇酯(56-a,3.6 g,產(chǎn)率73%)。產(chǎn)物經(jīng)1H-NMR(400 MHz,CD3OD)表征:δ 7.62(m,3H),1.35(s,12H)ppm。
參考文獻:
[1] Patent: US2015/336982, 2015, A1. Location in patent: Paragraph 0365; 0366; 0367
[2] Patent: WO2009/32861, 2009, A1. Location in patent: Page/Page column 45; 46
[3] Patent: WO2010/59658, 2010, A1. Location in patent: Page/Page column 149