154590-35-9
154590-35-9 結(jié)構(gòu)式
基本信息
3-Fluoro-4-[4-(Boc-amino)piperidino]aniline
4-(4-Amino-2-fluorophenyl)-1-Boc-piperazine
4-(4-Boc-piperazin-1-yl)-3-fluoroaniline ISO 9001：2015 REACH
4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester
1-Piperazinecarboxylic acid, 4-(4-amino-2-fluorophenyl)-, 1,1-dimethylethyl ester
物理化學(xué)性質(zhì)
制備方法
154590-34-8
154590-35-9
3-4-2: [3-Fluoro-4-(Boc-piperazinyl)]aniline的制備 向150 mL乙酸乙酯中依次加入9.3 g (28.6 mmol) 由制備實施例3-4-1合成的4-(2-氟-4-硝基苯基)哌嗪-1-羧酸叔丁酯和930 mg (10 wt%) Pd/C催化劑。將混合物置于氫氣反應(yīng)器中，在4 bar氫氣壓力下反應(yīng)6小時。反應(yīng)完成后，通過過濾移除Pd/C催化劑。濾液經(jīng)減壓蒸餾濃縮，隨后在約40℃下真空干燥，得到8.22 g (產(chǎn)率：97%) 標(biāo)題化合物。 質(zhì)譜(M + H)+: 296.11 1H-NMR (DMSO-d6) δ: 1.42 (s, 9H), 2.76 (br m, 4H), 3.43 (br m, 4H), 5.02 (s, 2H), 6.33 (m, 2H), 6.79 (m, 1H)。
參考文獻(xiàn)：
[1] Patent: US2011/306606, 2011, A1. Location in patent: Page/Page column 15
[2] Patent: EP2394993, 2011, A2. Location in patent: Page/Page column 23
[3] Patent: WO2005/82892, 2005, A2. Location in patent: Page/Page column 62-63
[4] Patent: WO2004/18439, 2004, A1. Location in patent: Page 31
[5] Patent: US2007/100141, 2007, A1. Location in patent: Page/Page column 27