66491-03-0

基本信息
7-氨基-3,4-二氫異喹啉-1(2H)-酮
7-氨基-3,4-二氫-2H-異喹啉-1-酮
66491-03-0 7-氨基-3,4-二氫異喹啉-1(2H)-酮
7-AMINO-3,4-DIHYDRO-2H-ISOQUINOLIN-1-ONE
7-Amino-3,4-dihydro-1(2H)-isoquinolinone
1(2H)-Isoquinolinone, 7-aMino-3,4-dihydro-
2-Propenoicacid,2-methyl-,2-(4-hydroxyethoxy)ethylester
物理化學性質
制備方法

22245-96-1

66491-03-0
以7-硝基-3,4-二氫異喹啉-1(2H)-酮為原料合成7-氨基-3,4-二氫異喹啉-1(2H)-酮的一般步驟:將7-硝基-3,4-二氫異喹啉-1(2H)-酮(700mg,3.6mmol)溶于甲醇(25mL)中,加入10%鈀/碳催化劑(催化量)。在氫氣(60psi)氛圍下攪拌反應1小時。反應完成后,將混合物通過硅藻土過濾以去除催化劑,濾液經真空濃縮得到7-氨基-3,4-二氫異喹啉-1(2H)-酮(500mg,收率86%)。產物經1H NMR(400MHz,CD3OD)表征:δ 2.81(t,J = 6.59Hz,2H),3.42(t,J = 6.55Hz,2H),6.84(dd,J = 8.13,2.42Hz,1H),7.02(d,J = 7.91Hz,1H),7.26(d,J = 2.64Hz,1H)。
參考文獻:
[1] Journal of Organic Chemistry, 1983, vol. 48, # 19, p. 3220 - 3234
[2] Patent: WO2008/79759, 2008, A1. Location in patent: Page/Page column 98
[3] Patent: WO2008/79836, 2008, A2. Location in patent: Page/Page column 86
[4] Journal of Medicinal Chemistry, 2015, vol. 58, # 6, p. 2799 - 2808
[5] ACS Medicinal Chemistry Letters, 2016, vol. 7, # 12, p. 1077 - 1081