1220220-21-2

基本信息
2-乙酰氨基-吡啶-4-硼酸頻哪醇酯
N-(4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)吡啶-2-基)乙酰胺
(2-acetamidopyridin-4-yl)boronic acid pinacol ester
N-[4-(tetraMethyl-1,3,2-dioxaborolan-2-yl)pyridin-2- yl]acetaMide
N-(4-(4,4,5,5-TetraMethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)acetaMide
Acetamide, N-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinyl]-
N-(4-(4,4,5,5-TetraMethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)acetaMide ISO 9001:2015 REACH
物理化學(xué)性質(zhì)
常見問題列表

1026796-81-5

73183-34-3

1220220-21-2
一般步驟:向裝有磁力攪拌器、溫度計(jì)、回流冷凝管和鼓泡器的1L四頸燒瓶中加入55.91g(0.26mol)N-(4-溴吡啶-2-基)乙酰胺和66.02g(0.26mol)聯(lián)硼酸頻那醇酯,隨后加入76.44g(0.78mol)醋酸鉀和450mL二惡烷,攪拌混合。在氮?dú)獗Wo(hù)下,加入3.81g(0.0051mol)二氯二茂鈀,升溫至100℃反應(yīng)18至24小時(shí),通過薄層色譜(TLC)監(jiān)測(cè)反應(yīng)進(jìn)度。反應(yīng)完成后,冷卻至室溫,析出固體,進(jìn)行打漿處理并過濾。將濾渣用500mL甲醇溶解,再次過濾,濾液蒸發(fā)至干。最后,加入庚烷進(jìn)行打漿,得到62.08g目標(biāo)產(chǎn)物2-乙酰氨基吡啶-4-硼酸頻那醇酯,收率為91.1%。
參考文獻(xiàn):
[1] Patent: CN103601745, 2017, B. Location in patent: Paragraph 0025; 0026
[2] Angewandte Chemie - International Edition, 2016, vol. 55, # 36, p. 10890 - 10894
[3] Angew. Chem., 2016, vol. 128, p. 11050 - 11054,5
[4] Journal of Medicinal Chemistry, 2017, vol. 60, # 13, p. 5613 - 5637
[5] Patent: US2013/165464, 2013, A1. Location in patent: Paragraph 0835