1021918-86-4
1021918-86-4 结构式
基本信息
5-(4,4,5,5-四甲基-1,3,2-二氧硼杂环戊烷-2-基)-1H-苯并[D]咪唑-1-甲酸叔丁酯
1H-苯并咪唑-1-甲酸, 5-(4,4,5,5-四甲基-1,3,2-二氧杂环己硼烷-2-基)-, 1,1-二甲基乙酯
tert-butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzimidazole-1-carboxylate
tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazole-1-carboxylate
tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzo[d]imidazole-1-carboxylate
1H-BenziMidazole-1-carboxylic acid, 5-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-, 1,1-diMethylethyl ester
物理化学性质
制备方法
942590-05-8
73183-34-3
1021918-86-4
1. 将5-溴-1H-苯并[d]咪唑-1-甲酸叔丁酯(10.2 mmol)、联硼酸频那醇酯(11.2 mmol)、乙酸钯(II)(1.02 mmol)、二氯[1,1'-二(二苯基膦基)二茂铁]钯(II)(1.02 mmol)和乙酸钾(30.4 mmol)在1,4-二恶烷(50 mL)和三乙胺(2 mL)的混合溶液中混合。2. 将反应混合物在110℃下加热过夜。3. 反应完成后,将混合物在真空下浓缩。4. 残余物通过快速色谱法(洗脱剂:10%乙酸乙酯/石油醚)纯化,得到目标产物5-(4,4,5,5-四甲基-1,3,2-二氧硼杂环戊烷-2-基)-1H-苯并[d]咪唑-1-甲酸叔丁酯,为固体,收率42%。
参考文献:
[1] Patent: WO2011/66211, 2011, A1. Location in patent: Page/Page column 71
[2] Patent: WO2009/7751, 2009, A2. Location in patent: Page/Page column 120-121
[3] Patent: WO2008/51493, 2008, A2. Location in patent: Page/Page column 151
[4] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 22, p. 6793 - 6799
[5] Patent: WO2013/28445, 2013, A1. Location in patent: Page/Page column 56; 57
