659729-09-6
659729-09-6 結(jié)構(gòu)式
基本信息
PYRIMIDINE, 4-CHLORO-6-[4-(TRIFLUOROMETHYL)PHENYL]-
物理化學(xué)性質(zhì)
制備方法
1193-21-1
128796-39-4
659729-09-6
一般步驟:所有用于該反應(yīng)的溶劑和溶液需用氬氣脫氣15分鐘。在氬氣保護(hù)下,于圓底燒瓶中將4,6-二氯嘧啶(1.5當(dāng)量)溶解于THF(1M)中。隨后加入4-三氟甲基苯硼酸(1.0當(dāng)量)、乙酸鈀(0.02當(dāng)量,2mol%)、三苯基膦(0.04當(dāng)量,4mol%)及1M Na2CO3水溶液(2.0當(dāng)量)。將反應(yīng)混合物在60°C下攪拌過夜。反應(yīng)完成后,冷卻至室溫,用水層和Et2O進(jìn)行萃取。合并有機(jī)層,用鹽水洗滌,無水MgSO4干燥,過濾并減壓濃縮。粗產(chǎn)物通過快速柱色譜法純化,得到目標(biāo)化合物4-氯-6-(4-(三氟甲基)苯基)嘧啶。
參考文獻(xiàn):
[1] Bioorganic and Medicinal Chemistry Letters, 2017, vol. 27, # 2, p. 299 - 302
[2] Patent: CN106632488, 2017, A. Location in patent: Paragraph 0167-0169
[3] Journal of Medicinal Chemistry, 2007, vol. 50, # 15, p. 3497 - 3514
[4] Patent: US2006/241296, 2006, A1. Location in patent: Page/Page column 27
[5] Patent: WO2010/134478, 2010, A1. Location in patent: Page/Page column 165
