5-溴-2,3-二氫異吲哚-1-酮為酮類衍生物,可用作醫(yī)藥中間體,如可用于制備苯并氮雜卓衍生物。
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以4-溴-2-溴甲基苯甲酸甲酯為原料合成5-溴-2,3-二氫異吲哚-1-酮的一般步驟如下:將4-溴-2-溴甲基苯甲酸甲酯(3.70 g)懸浮于2M氨的甲醇溶液(36 mL)和濃氫氧化銨(12 mL)中,反應(yīng)18小時(shí)。反應(yīng)完成后,過濾收集固體產(chǎn)物,得到5-溴-2,3-二氫異吲哚-1-酮,為無色固體(2.3 g,收率90%)。產(chǎn)物經(jīng)1H NMR(300 MHz,CDCl3)表征:δ 7.68(m,3H),4.44(s,2H)。
參考文獻(xiàn):
[1] Patent: WO2006/20879, 2006, A1. Location in patent: Page/Page column 66-67
[2] Patent: WO2015/52264, 2015, A1. Location in patent: Paragraph 0637; 0638
[3] Patent: WO2008/23161, 2008, A1. Location in patent: Page/Page column 121
[4] Patent: WO2005/73205, 2005, A1. Location in patent: Page/Page column 25
[5] Patent: US2007/49603, 2007, A1. Location in patent: Page/Page column 91-92