130966-46-0

基本信息
(2S,3R)-1-BOC-3-羥基吡咯烷-2-甲酸甲酯
2-甲基-3-羥基吡咯烷-1,2-二羧酸-(2S,3R)-1-叔丁酯
(2S,3R)-1-叔丁基 2-甲基 3-羥基吡咯烷-1,2-二羧酸酯
1-叔-丁基 2-甲基 (2S,3R)-3-羥基吡咯烷-1,2-二甲酸基酯
-1-tert-Butyl 2-methyl 3-hydroxypyrrolidine-1,2-dicarboxylate
1-tert-butyl 2-methyl (2S,3R)-3-hydroxypyrrolidine-1,2-dicar...
(2S,3R)-N-tert-Butoxycarbonyl-3-hydroxy-2-pyrrolidinecarboxylic
1-tert-butyl 2-methyl (2S,3R)-3-hydroxypyrrolidine-1,2-dicarboxylate
(2S,3R)-1-tert-Butyl-2-methyl-3-hydroxypyrrolidine-1,2-dicarboxylate
(2S,3R)-1-(tert-BOC)-3-Hydroxypyrrolidine-2-carboxylic acid methyl ester
(2S,3R)-N-tert-Butoxycarbonyl-3-hydroxy-2-pyrrolidinecarboxylic acid Methyl ester
(2S,3R)-1-(tert-Butoxycarbonyl)-3-Hydroxypyrrolidine-2-carboxylic acid Methyl ester
1,2-Pyrrolidinedicarboxylic acid, 3-hydroxy-, 1-(1,1-dimethylethyl) 2-methyl ester, (2S,3R)-
物理化學(xué)性質(zhì)
制備方法

496841-07-7

130966-46-0
以(2S,3R)-N-叔丁氧羰基-3-苯甲酰氧基-2-吡咯烷甲酸甲酯為原料合成N-Boc-(2S,3R)-3-羥基吡咯烷-2-羧酸甲酯的一般步驟如下:將(2S,3R)-N-叔丁氧羰基-3-苯甲酰氧基-2-吡咯烷甲酸甲酯(2.3 g,6.58 mmol)溶解于甲醇(20 mL)中,冰浴冷卻至0℃。緩慢滴加1 mol/L氫氧化鉀水溶液(7.3 mL),保持反應(yīng)溫度在0℃,攪拌反應(yīng)1小時。反應(yīng)完成后,向反應(yīng)混合物中加入5%硫酸氫鉀水溶液調(diào)節(jié)pH至酸性,隨后用乙酸乙酯進行萃取。合并有機層,用飽和氯化鈉水溶液洗滌,無水硫酸鈉干燥,過濾。濾液經(jīng)減壓濃縮后,所得殘余物通過硅膠柱色譜法純化,得到目標產(chǎn)物N-Boc-(2S,3R)-3-羥基吡咯烷-2-羧酸甲酯(1.55 g,收率78%)。質(zhì)譜(ESI+)顯示分子離子峰m/z 246([M+H]+,相對豐度0.5%)。
參考文獻:
[1] Journal of Medicinal Chemistry, 2006, vol. 49, # 26, p. 7596 - 7599
[2] Patent: EP2876105, 2015, A1. Location in patent: Paragraph 1151; 1152
[3] Journal of Medicinal Chemistry, 2007, vol. 50, # 13, p. 3015 - 3025
[4] Patent: US2005/197359, 2005, A1. Location in patent: Page/Page column 17