938043-30-2

基本信息
4-(4-甲基-1-哌嗪甲基)苯硼酸频哪酯
4-(4-甲基-1-哌嗪甲基)苯硼酸频哪酯,95%
1-甲基-4-[4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)苄基]哌嗪
4-[(4-Methylpiperazin-1-yl)methyl]benzeneboronicacidpinacolester
4-((4-Methylpiperazin-1-yl)methyl)-phenylboronic acid pinacol ester
4-(4-METHYL-1-PIPERAZINYLMETHYL)BENZENEBORONIC ACID PINACOL ESTER,95%
4-(4-Methyl-1-piperazinylmethyl)benzeneboronic acid pinacol ester, 95%
1-Methyl-4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperazine
1-methyl-4-{[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methyl}piperazine
1-Methyl-4-[[4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)phenyl]Methyl]piperazine
物理化学性质
制备方法
![1-[(4-BROMOPHENYL)METHYL]-4-METHYLPIPERAZINE](/CAS/GIF/368879-17-8.gif)
368879-17-8

73183-34-3

938043-30-2
在室温下,向搅拌的1-[(4-溴苯基)甲基]-4-甲基哌嗪(35.0g,130mmol)的1,4-二恶烷(500mL)溶液中加入乙酸钾(38.3g,390mmol)和联硼酸频那醇酯(33.0g,130mmol)。将混合物进行抽真空并用氮气置换(重复三次)。加入Pd(dppf)Cl2(3.0g,1.3mmol)后,将反应混合物在110℃下于氮气氛围中搅拌12小时。反应完成后,将混合物冷却至室温,过滤除去固体。浓缩滤液,残余物用乙酸乙酯和水进行稀释。分离有机层,用无水Na2SO4干燥后浓缩。通过硅胶快速柱色谱法(洗脱剂比例:DCM/MeOH = 50:1至10:1)纯化残余物,得到4-(4-甲基-1-哌嗪甲基)苯硼酸频哪酯(37.0g,产率90%),为棕色固体。
参考文献:
[1] Patent: WO2015/32945, 2015, A1. Location in patent: Page/Page column 26; 27
[2] Patent: US2018/44328, 2018, A1. Location in patent: Paragraph 0162; 0174; 0175
[3] Patent: WO2012/119941, 2012, A1. Location in patent: Page/Page column 116
[4] Journal of Medicinal Chemistry, 2008, vol. 51, # 2, p. 196 - 218
[5] European Journal of Medicinal Chemistry, 2016, vol. 122, p. 684 - 701