142253-50-7

基本信息
(S)-1-Boc-2-(cyanomethyl)pyrrolidine
(S)-TERT-BUTYL 2-(CYANOMETHYL)PYRROLIDINE-1-CARBOXYLATE
tert-butyl (2S)-2-(cyanomethyl)pyrrolidine-1-carboxylate
2-(cyanomethyl)-1-pyrrolidinecarboxylic acid tert-butyl ester
1-Pyrrolidinecarboxylic acid, 2-(cyanoMethyl)-, 1,1-diMethylethyl ester, (2S)-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表

773837-37-9

86661-32-7

142253-50-7
以化合物(CAS: 773837-37-9)和(S)-2-((甲苯磺酰氧基)甲基)吡咯烷-1-甲酸叔丁酯為原料,合成(S)-2-(氰基甲基)吡咯烷-1-甲酸叔丁酯的一般步驟如下:向中間體6(90.4 g,255 mmol)的二甲基亞砜(255 mL)溶液中加入氰化鈉(16.2 g,331 mmol),并將混合物加熱至100℃。反應(yīng)混合物在100℃下攪拌4小時(shí)后,冷卻至室溫,加入水稀釋。水層用乙酸乙酯萃取,合并有機(jī)層。有機(jī)層依次用水和飽和鹽水洗滌,然后用無(wú)水硫酸鈉干燥。干燥后的有機(jī)相在減壓下濃縮,得到粗產(chǎn)物。粗產(chǎn)物通過(guò)硅膠柱色譜法純化,洗脫劑為石油醚/乙酸乙酯(70/30至30/70,v/v),得到(S)-2-(氰基甲基)吡咯烷-1-甲酸叔丁酯(35.2 g,168 mmol,產(chǎn)率66%)。質(zhì)譜(ESI+)顯示分子離子峰m/z 211([M+H]+,100%)。
參考文獻(xiàn):
[1] Patent: WO2011/111875, 2011, A1. Location in patent: Page/Page column 63-64
[2] Patent: WO2012/154676, 2012, A1. Location in patent: Page/Page column 180
[3] Patent: WO2014/71368, 2014, A1. Location in patent: Paragraph 00410
[4] Patent: WO2016/196393, 2016, A2. Location in patent: Paragraph 00277