1421372-94-2
1421372-94-2 結(jié)構(gòu)式
基本信息
甲磺酸奧希替尼中間體
AZD9291中間體2
AZD-9291中間體一
AZD9291 N-4步中間體
N-(2-甲氧基-4-氟-5-硝基苯基)-4-(1-甲基-3-吲哚基)-2-嘧啶胺
N-(4-氟-2-甲氧基-5-硝基苯基)-4-(1-甲基吲唑-3-基)嘧啶-2-胺
N-(4-氟-2-甲氧基-5-硝基-苯基)-4-(1-甲基吲哚-3-基)-嘧啶-2-胺
(4-氟-2-甲氧基-5-硝基苯基)-4-(1-甲基-1H-吲哚-3-基)-2-嘧啶胺
N-(4-氟-2-甲氧基-5-硝基苯基)-4-(1-甲基-1H-吲哚-3-基)嘧啶-2-胺
EOS-61221
AZD9291 N-3
AZD9291 Intermediate 2
OSIMERTINIB INTERMEDIATE 1
Osimertinib mesylate intermediate 1
N-(4-Fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-3-indolyl)-2-pyrimidinamine
N-(4-fluoro-2-Methoxy-5-nitrophenyl)-4-(1-Methylindol-3-yl)pyriMidin-2-aMine
N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine
N-(4-Fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)-2-pyrimidinamine
物理化學(xué)性質(zhì)
制備方法
1032452-86-0
1075705-01-9
1421372-94-2
在室溫下，向2L三口燒瓶中加入1000mL 2-戊醇，50g 3-(2-氯嘧啶-4-基)-1-甲基吲哚，42g 4-氟-2-甲氧基-5-硝基苯胺，3.54g對(duì)甲苯磺酸。將反應(yīng)混合物加熱至80℃并保持?jǐn)嚢璺磻?yīng)6小時(shí)。反應(yīng)完成后，將混合物冷卻至25℃至28℃，隨后過(guò)濾收集固體產(chǎn)物。濾餅用預(yù)熱的2-戊醇（50℃）洗滌，以去除雜質(zhì)。將所得固體產(chǎn)物置于真空烘箱中干燥，最終得到80.1g黃色固體產(chǎn)物N-(4-氟-2-甲氧基-5-硝基苯基)-4-(1-甲基-1H-吲哚-3-基)嘧啶-2-胺，收率為99.0%。
參考文獻(xiàn)：
[1] Patent: CN107188888, 2017, A. Location in patent: Paragraph 0061-0063
[2] European Journal of Medicinal Chemistry, 2017, vol. 135, p. 12 - 23
[3] Patent: WO2013/14448, 2013, A1. Location in patent: Page/Page column 138
[4] Journal of Medicinal Chemistry, 2014, vol. 57, # 20, p. 8249 - 8267
[5] Patent: CN107043369, 2017, A. Location in patent: Paragraph 0395; 0396; 0397; 0398