39945-51-2

基本信息
1-CBZ-3-HYDROXYMETHYL-PIPERIDINE
3-HYDROXYMETHYL-PIPERIDINE-1-CARBOXYLIC ACID BENZYL ESTER
BENZYL 3-(HYDROXYMETHYL)PIPERIDINE-1-CARBOXYLATE
BENZYL 3-(HYDROXYMETHYL)TETRAHYDRO-1(2H)-PYRIDINECARBOXYLATE
BUTTPARK 75\50-54
N-Cbz-3-hydroxymethylpiperidine
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見問題列表

4606-65-9

501-53-1

39945-51-2
向3-羥甲基哌啶(0.61 g, 5 mmol)的二氯甲烷(10 mL)冷凍溶液中加入三乙胺(0.51 g, 5 mmol),隨后緩慢滴加氯甲酸芐酯(0.88 g, 5 mmol)。將反應(yīng)混合物逐漸升溫至室溫并持續(xù)攪拌過夜。反應(yīng)完成后,加入二氯甲烷(50 mL)稀釋反應(yīng)混合物,依次用5%鹽酸溶液(2 × 20 mL)、飽和碳酸氫鈉溶液(20 mL)和飽和氯化鈉溶液(20 mL)洗滌有機(jī)層。有機(jī)層經(jīng)無(wú)水硫酸鈉干燥后,過濾除去干燥劑,減壓濃縮去除溶劑。粗產(chǎn)物通過快速柱色譜法(硅膠,乙酸乙酯/己烷為洗脫劑)純化,得到目標(biāo)化合物3-甲醇-N-芐氧羰基哌啶(1.21 g, 收率96%),為無(wú)色油狀物。1H NMR (CDCl3) δ: 1.20-1.83 (m, 5H), 2.78-3.20 (m, 2H), 3.50 (s, 2H), 3.69-4.05 (m, 2H), 5.14 (s, 2H), 7.25-7.40 (m, 5H)。
參考文獻(xiàn):
[1] Bioorganic and Medicinal Chemistry, 2011, vol. 19, # 20, p. 5975 - 5983
[2] Journal of Medicinal Chemistry, 2006, vol. 49, # 9, p. 2673 - 2676
[3] Patent: WO2005/806, 2005, A2. Location in patent: Page 85
[4] Patent: US2010/48606, 2010, A1. Location in patent: Page/Page column 32
[5] Patent: EP1780210, 2007, A1. Location in patent: Page/Page column 51