37813-30-2

基本信息
1-叔丁氧羰基-4-羥基-L-脯氨酸乙酯
1-叔丁氧羰基-4R-羥基-L-脯氨酸乙酯
1-叔丁氧羰基-(4R)-羥基-2-脯氨酸乙酯
1-叔丁氧羰基-(4R)-羥基-2-脯氨酸乙脂
(2S,4R)-1-BOC-2-甲酸乙酯-4-羥基吡咯烷
Boc-L-Hyp-oet
Boc-L-Hydroxy-Proline Ethyl Ester
1-Boc-L-hydroxyproline ethyl ester
1-Boc-4-Hydroxy-L-Proline Ethyl Ester
(Tert-Butoxy)Carbonyl Hyp-OEt (Syrup)
(4R)-1-Boc-4-hydroxy-L-proline ethyl ester
1-tert-butoxycarbonyl-4-hydroxy-L-proline ethyl ester
1-tert-Butoxycarbonyl-4R-hydroxy-L-proline ethyl ester
1-tert-butoxycarbonyl-4-hydroxy-L-proline ethyl ester USP/EP/BP
物理化學(xué)性質(zhì)
制備方法

24424-99-5

33996-30-4

37813-30-2
步驟2:將(2S,4R)-4-羥基吡咯烷-2-甲酸乙酯鹽酸鹽(146.2 g,0.747 mol)溶解于二氯甲烷(1600 mL)和乙醇(100 mL)的混合溶劑中,冷卻至0℃。在攪拌下,向該溶液中加入三乙胺(113.4 g,1.12 mol,156.2 mL)。隨后,分批加入二碳酸二叔丁酯(195.6 g,0.90 mol)。反應(yīng)混合物在0℃下攪拌15分鐘,然后升至室溫繼續(xù)攪拌16小時。反應(yīng)完成后,將混合物濃縮至約800 mL,用水洗滌。有機(jī)層用硫酸鎂干燥,過濾后濃縮。通過硅膠柱色譜法(洗脫劑:20%乙酸乙酯-二氯甲烷)純化,得到Boc-L-羥脯氨酸乙酯(193.7 g,100%)為黃色油狀物。質(zhì)譜(M + Na):m/e 282。1H-NMR(CDCl3)δ 1.30(t,3H),1.45(s,9H),1.75(m,1H),2.10(m,1H),2.30(m,1H),3.45和3.55(d,1H,兩個旋轉(zhuǎn)異構(gòu)體),3.65(dd,1H),4.25(m,2H),4.40和4.45(t,1H,兩個旋轉(zhuǎn)異構(gòu)體),4.55(寬s,1H)。
參考文獻(xiàn):
[1] Patent: WO2008/8327, 2008, A2. Location in patent: Page/Page column 15-16
[2] Patent: US2011/3780, 2011, A1. Location in patent: Page/Page column 4
[3] Journal of Heterocyclic Chemistry, 2011, vol. 48, # 5, p. 1132 - 1139
[4] Patent: TW2017/8221, 2017, A. Location in patent: Page/Page column 38
[5] Synlett, 2011, # 14, p. 2059 - 2063