160809-38-1

基本信息
1-CBZ-4-哌啶甲酸乙酯
1-CBZ-哌啶-4-甲酸乙酯
1-芐氧羰基哌啶-4-羧酸乙酯
N-CBZ-4-哌啶甲酸乙酯98%
1-芐基4-乙基哌啶-1,4-二羧酸酯
1-CBZ-4-哌啶甲酸乙酯 50G左右
N-CBZ-4-哌啶甲酸乙酯 98% 50G
N-CBZ-4-哌啶甲酸乙酯(CAS號:160809-38-1)
N-CBZ-4-哌啶甲酸乙酯,(R)-3-哌啶甲酸乙酯,(R)-3-哌啶甲酸乙酯-L-酒石酸鹽
1-BENZYL 4-ETHYL PIPERIDINE-1,4-DICARBOXYLATE
1-O-benzyl 4-O-ethyl piperidine-1,4-dicarboxylate
Piperidine derivative Ethyl-N-CBZ-piperidine-4-carboxylate
1,4-Piperidinedicarboxylic acid, 4-ethyl 1-(phenylMethyl) ester
piperidine-1,4-dicarboxylic acid O4-ethyl ester O1-(phenylmethyl) ester
Piperidine derivative CAS NO.160809-38-1 Ethyl-N-CBZ-piperidine-4-carboxylate
物理化學(xué)性質(zhì)
制備方法

1126-09-6

501-53-1

160809-38-1
以4-哌啶甲酸乙酯和氯甲酸芐酯為原料合成1-Cbz-哌啶-4-甲酸乙酯的一般步驟如下:在冰浴冷卻條件下,將氯甲酸芐酯(95 g,0.56 mol)的二氯甲烷(200 mL)溶液緩慢滴加到攪拌中的4-哌啶甲酸乙酯(87 g,0.55 mol)和碳酸鈉(60 g,0.57 mol)的混合物中。滴加過程控制在70分鐘內(nèi)完成,期間同時加入二氯甲烷(200 mL)。反應(yīng)混合物在室溫下持續(xù)攪拌2.5天,隨后通過Celte墊過濾。濾液經(jīng)真空濃縮后,將殘余物在2M鹽酸水溶液和乙醚之間進(jìn)行分配。分離有機(jī)層,用無水硫酸鎂干燥,過濾并濃縮。最后,通過硅膠柱色譜法(洗脫劑:乙酸乙酯/異己烷)純化殘余物,得到目標(biāo)產(chǎn)物1-Cbz-哌啶-4-甲酸乙酯(152 g,產(chǎn)率94%)。產(chǎn)物經(jīng)1H NMR(360 MHz,CDCl3)表征:δ 7.40-7.27(5H,m),5.12(2H,s),4.22-3.99(2H,m),4.40(2H,q,J=7.4 Hz),2.93(2H,br t,J=11.6 Hz),2.45(2H,m),1.97-1.81(2H,m),1.74-1.56(2H,m),1.25(3H,t,J=7.4 Hz)。
參考文獻(xiàn):
[1] Patent: WO2004/78750, 2004, A1. Location in patent: Page 64
[2] Patent: US2006/229289, 2006, A1. Location in patent: Page/Page column 21
[3] Patent: WO2007/93603, 2007, A1. Location in patent: Page/Page column 15
[4] Patent: EP1522540, 2005, A1. Location in patent: Page/Page column 63
[5] Patent: WO2015/118342, 2015, A1. Location in patent: Page/Page column 67; 68