91419-49-7

基本信息
N-BOC-3-哌啶甲酰胺
1-BOC-哌啶-3-甲酰胺
1-叔丁氧羰基哌啶-3-甲酰胺
1-叔丁氧羰基-3-哌啶甲酰胺
1-BOC-3-氨基甲酰基哌啶
1-N-BOC-哌啶-3-甲酰胺
N-BOC-3-哌啶甲酰胺(1-BOC-哌啶-3-甲酰胺)
BOC-3-Piperidine carboxamide
1-N-BOC-3-CARBAMOYLPIPERIDINE
N-BOC-3-PiperidineCarboxamide
1-Boc-3-piperidinecarboxamide
1-Boc-piperidine-3-carboxamide
N-BOC-piperidine-3-carboxamide
1-N-Boc-3-piperidinecarboxamide
1-N-BOC-PIPERIDINE-3-CARBOXAMIDE
1-Boc-3-(aMinocarbonyl)-piperidine
物理化學(xué)性質(zhì)
制備方法

71381-75-4

91419-49-7
以1-BOC-哌啶-3-羧酸為原料合成N-BOC-3-哌啶甲酰胺的一般步驟:在0℃及氮?dú)獗Wo(hù)下,向1-Boc-哌啶-3-羧酸(1.58g,6.89mmol)的氯仿溶液(10mL)中逐滴加入三乙胺(0.96mL,6.89mmol)和氯甲酸乙酯(0.69mL,7.23mmol)。反應(yīng)混合物在0℃下攪拌10分鐘后,通入氨氣(氣體)1小時(shí)。隨后,將反應(yīng)混合物升溫至室溫并繼續(xù)攪拌3小時(shí)。反應(yīng)完成后,加入5%碳酸氫鈉水溶液,分離有機(jī)相和水相。有機(jī)層用無(wú)水硫酸鈉干燥,減壓濃縮,得到粗品N-BOC-3-哌啶甲酰胺,無(wú)需進(jìn)一步純化即可用于后續(xù)反應(yīng)。產(chǎn)量:定量;LCMS(保留時(shí)間):3.31分鐘(方法A);質(zhì)譜(電噴霧正離子模式)顯示m/z:229.0([M+H]+)。
參考文獻(xiàn):
[1] Patent: WO2006/123257, 2006, A2. Location in patent: Page/Page column 34
[2] Patent: US8080566, 2011, B1. Location in patent: Page/Page column 37-38
[3] European Journal of Medicinal Chemistry, 1984, vol. 19, # 2, p. 181 - 186
[4] Journal of Medicinal Chemistry, 2007, vol. 50, # 9, p. 2225 - 2239
[5] Patent: WO2014/149164, 2014, A1. Location in patent: Paragraph 00605