1372540-25-4

基本信息
2-甲基-1-[[2-甲基-3-(三氟甲基)苯基]甲基]-6-(4-吗啉基)-1H-苯并咪唑-4-羧酸
GSK2636771
GSK 2636771B
GSK2636771cas
GSK2636771 USP/EP/BP
GSK2636771/GSK-2636771
GSK 2636771 dihydrochloride
PI3Kβ-selective inhibitor GS2636771
2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic
2-METHYL-1-[[2-METHYL-3-(TRIFLUOROMETHYL)PHENYL]METHYL]-6-MORPHOLIN-4-YLBENZIMIDAZOLE-4-CARBOXYLIC ACID
物理化学性质
制备方法
![methyl 2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxy](/CAS/20180808/GIF/1372540-24-3.gif)
1372540-24-3

1372540-25-4
以2-甲基-1-{[2-甲基-3-(三氟甲基)苯基]甲基}-6-(4-吗啉基)-1H-苯并咪唑-4-羧酸酯(180mg,0.4mmol)为原料,将其溶解于THF(10mL)中。向此溶液中加入2N LiOH水溶液(1.2mL),随后在50℃下搅拌反应1小时。通过TLC监测反应进程,确认原料完全消耗后,将反应混合物冷却至室温。在减压条件下除去THF,随后将混合物pH值调节至3进行酸化。将所得悬浮液过滤,滤饼用水(10mL)洗涤,最终得到白色固体产物2-甲基-1-[[2-甲基-3-(三氟甲基)苯基]甲基]-6-(4-吗啉基)-1H-苯并咪唑-4-羧酸(152mg,收率)。产物经1H NMR(300MHz,DMSO-d6)表征:δ 2.46(s,3H),2.54(s,3H),3.10(t,4H,J = 4.8Hz),3.73(t,4H,J = 4.8Hz),5.63(s,2H),6.37(d,1H,J = 7.8Hz),7.26(t,1H,J = 7.8Hz),7.35(d,1H,J = 2.4Hz),7.44(d,1H,J = 2.4Hz),7.62(d,1H,J = 7.8Hz);LC-MS:m/e = 434 [M + 1]+。
参考文献:
[1] Patent: US2012/88767, 2012, A1. Location in patent: Page/Page column 35
[2] Patent: US2016/287610, 2016, A1. Location in patent: Paragraph 0054; 0055
[3] Patent: WO2015/42029, 2015, A1. Location in patent: Page/Page column 17
常见问题列表
Target | Value |
PI3Kβ |
GSK-2636771对PTEN缺失细胞系(人前列腺癌PC-3和乳腺癌HCC70)具有选择性抑制活性,EC50分别为36 nM 和 72 nM。