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| (S)-4-氨基-1-甲基吡咯烷-2-酮的合成 | |
| 引用本文： | 邵怀启,冯亚青,洪浩.(S)-4-氨基-1-甲基吡咯烷-2-酮的合成[J].精细化工,2008,25(7). |
| 作者姓名： | 邵怀启 冯亚青 洪浩 |
| 作者单位： | 1. 天津大学化工学院,天津,300072;凯莱英医药化学(天津)有限公司,天津,300457 2. 天津大学化工学院,天津,300072 3. 凯莱英医药化学(天津)有限公司,天津,300457 |
| 摘 要： | (S)-4-氨基-1-甲基吡咯烷-2-酮是合成杂环类镇痛药的重要中间体。以L-天冬氨酸为起始原料,经5步反应合成了(S)-4-氨基-1-甲基吡咯烷-2-酮,总收率19%。对合成路线中的关键步骤——双内酰胺的还原过程进行了量子化学计算,并以硼氢化钠/硫酸为还原剂,实现了双内酰胺的单羰基还原过程,还原反应收率90%,区域选择性100%。该路线已实现千克级生产,生产总收率17%。 |
| 关 键 词： | 吡咯烷酮 区域选择性还原 双内酰胺 量子化学 医药与日化原料 |
Synthesis of (S)-4-Amino-1-methylpyrrolidine-2-one |
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| SHAO Huai-qi,FENG Ya-qing,HONG Hao.Synthesis of (S)-4-Amino-1-methylpyrrolidine-2-one[J].Fine Chemicals,2008,25(7). | |
| Authors: | SHAO Huai-qi FENG Ya-qing HONG Hao |
| Abstract: | (S)-4-Amino-1-methylpyrrolidine-2-one,an important intermediate for synthesis of heterocyclic analgesics,was synthesized by 5 steps from L-aspartic acid with 19% total yield.The regioselective reduction process of the di-lactame as a key step was calculated by quantum chemistry and achieved by using sodium borohydride and sulfuric acid in 90% yield and 100% regioselectivity.The production of kilogram scale was achieved with 17% total yield. |
| Keywords: | pyrrolidone regioselective reduction di-lactame quantum chemistry drug and cosmetic materials |
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