503315-74-0

基本信息
3-氟-4-硝基苯甲醇
(3-氟-4-硝基苯基)甲醇
(3-Fluoro-4-nitrophenyl)
3-Fluoro-4-nitrobenzenemethanol
3-Fluoro-4-nitrobenzylalcohol98%
Benzenemethanol, 3-fluoro-4-nitro-
3-Fluoro-4-nitrobenzyl alcohol 99%
(3-Fluoro-4-nitrophenyl)methanol, 2-Fluoro-4-(hydroxymethyl)nitrobenzene
物理化學(xué)性質(zhì)
制備方法

403-21-4

503315-74-0
部分A. 制備(3-氟-4-硝基苯基)甲醇。在0℃下,向3-氟-4-硝基苯甲酸(2.0g,10.8mmol)的四氫呋喃(THF,50ml)溶液中逐滴加入硼烷-二甲硫醚絡(luò)合物(BH3-Me2S,2.215ml,22.15mmol)。將反應(yīng)混合物在0℃下攪拌3小時(shí),隨后升溫至65℃繼續(xù)攪拌18小時(shí)。反應(yīng)完成后,將混合物冷卻至室溫,緩慢加入冰(50g)淬滅反應(yīng),隨后加入1M鹽酸水溶液(100ml)。用乙酸乙酯(EtOAc,200ml)萃取反應(yīng)混合物,合并有機(jī)層,用無水硫酸鈉(Na2SO4)干燥,過濾后減壓濃縮,得到標(biāo)題化合物(3-氟-4-硝基苯基)甲醇,為白色固體(1.79g,收率97%)。
參考文獻(xiàn):
[1] Patent: WO2009/39135, 2009, A1. Location in patent: Page/Page column 140
[2] Journal of Medicinal Chemistry, 2018, vol. 61, # 3, p. 1153 - 1163
[3] Patent: WO2011/66416, 2011, A1. Location in patent: Page/Page column 16
[4] Patent: WO2004/7491, 2004, A1. Location in patent: Page 65
[5] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 13, p. 3986 - 3991