769944-78-7

基本信息
N-BOC-4-對溴苯基哌啶
1-N-BOC-4-對溴苯基哌啶
N-BOC-4-(4-溴苯基)哌啶
1-N-BOC-4-(4-溴苯基)哌啶
4-(4-溴苯基)哌啶-1-羧酸叔丁酯
1-N-叔丁氧羰基-4-(4-溴苯基)哌啶
1-Boc-4-(4-Bromo-phenyl)-piperidine
1-N-BOC-4-(4-BROMOPHENYL)PIPERIDINE
1-N-Boc-4-(5-Bromophenyl)piperidine
4-(N-Boc-piperidin-4-yl)bromobenzene
4-(4-BROMO-PHENYL)-PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER
1-Piperidinecarboxylic acid, 4-(4-bromophenyl)-, 1,1-dimethylethyl ester
物理化學(xué)性質(zhì)
制備方法

80980-89-8

24424-99-5

769944-78-7
部分A:在0℃條件下,將4-(4-溴苯基)哌啶(960mg, 4.0mmol)與二碳酸二叔丁酯(960mg, 4.4mmol)在二氯甲烷(DCM, 10mL)中混合。通過LC-MS分析確認(rèn)反應(yīng)完成后,加入額外的二氯甲烷(10mL)稀釋反應(yīng)混合物。隨后,用1N HCl(10mL)洗滌反應(yīng)混合物,以去除未反應(yīng)的原料和副產(chǎn)物。有機(jī)相用無水硫酸鎂干燥,過濾后濃縮。通過快速柱色譜法純化粗產(chǎn)物,采用梯度洗脫(0至100%己烷/乙酸乙酯)條件,得到目標(biāo)化合物1-N-Boc-4-(4-溴苯基)哌啶(化合物2),為白色固體(1.36g, 100%收率)。HPLC-MS分析顯示保留時(shí)間t R = 2.50min(UV檢測波長2*nm),質(zhì)量計(jì)算值為C16H22BrNO2[M+H]+ 339.1,實(shí)際觀察到的LCMS m/z為284.1(M+H-tBu)。
參考文獻(xiàn):
[1] Patent: WO2010/17060, 2010, A1. Location in patent: Page/Page column 31
[2] Patent: WO2009/158369, 2009, A1. Location in patent: Page/Page column 50
[3] Patent: WO2017/11776, 2017, A1. Location in patent: Paragraph 00698; 00699; 00700
[4] Patent: WO2007/70398, 2007, A1. Location in patent: Page/Page column 253
[5] Patent: WO2007/97937, 2007, A1. Location in patent: Page/Page column 188-189