1021918-86-4
1021918-86-4 結(jié)構(gòu)式
基本信息
5-(4,4,5,5-四甲基-1,3,2-二氧硼雜環(huán)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-1,3,2-二氧雜環(huán)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
物理化學(xué)性質(zhì)
制備方法
942590-05-8
73183-34-3
1021918-86-4
1. 將5-溴-1H-苯并[d]咪唑-1-甲酸叔丁酯(10.2 mmol)、聯(lián)硼酸頻那醇酯(11.2 mmol)、乙酸鈀(II)(1.02 mmol)、二氯[1,1'-二(二苯基膦基)二茂鐵]鈀(II)(1.02 mmol)和乙酸鉀(30.4 mmol)在1,4-二惡烷(50 mL)和三乙胺(2 mL)的混合溶液中混合。2. 將反應(yīng)混合物在110℃下加熱過(guò)夜。3. 反應(yīng)完成后,將混合物在真空下濃縮。4. 殘余物通過(guò)快速色譜法(洗脫劑:10%乙酸乙酯/石油醚)純化,得到目標(biāo)產(chǎn)物5-(4,4,5,5-四甲基-1,3,2-二氧硼雜環(huán)戊烷-2-基)-1H-苯并[d]咪唑-1-甲酸叔丁酯,為固體,收率42%。
參考文獻(xiàn):
[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
