| D-脯氨酰胺的合成新工艺 |
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| 引用本文： | 王蓓,许文松,栗更新,徐六兴. D-脯氨酰胺的合成新工艺[J]. 中国药物化学杂志, 2005, 15(5): 285-287 |
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| 作者姓名： | 王蓓 许文松 栗更新 徐六兴 |
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| 作者单位： | 浙江大学,材料与化工学院制药工程研究所,浙江,杭州,310027 |
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| 摘 要： | 目的研究手性中间体D-脯氨酰胺合成的新工艺.方法以L-脯氨酸为起始原料,S-酒石酸为拆分剂,运用不对称转换的方法合成D-脯氨酸.进一步应用手性源技术,经氨基保护、酯化、氨化和脱保护等步骤,不对称合成目标化合物.结果与结论目标化合物收率达到78.4%,光学纯度达到99.3%(以D-脯氨酸计).新工艺与专利文献相比,具有收率高,光学纯度好的特点,更适合工业化生产.
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| 关 键 词： | 药物化学 工艺改进 不对称合成 手性药物 D-脯氨酰胺 |
| 文章编号： | 1005-0108（2005）05-0285-03 |
| 收稿时间： | 2005-05-18 |
| 修稿时间： | 2005-05-18 |
New synthetic route for D-prolinamide |
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| WANG Bei,XU Wen-song,LI Geng-xin,XU Liu-xing. New synthetic route for D-prolinamide[J]. Chinese Journal of Medicinal Chemistry, 2005, 15(5): 285-287 |
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| Authors: | WANG Bei XU Wen-song LI Geng-xin XU Liu-xing |
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| Affiliation: | Institute of Pharmaceutical Engineering, College of Materials Science and Chemical Engineering, Zhejiang University, Hangzhou 310027, China |
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| Abstract: | Aim To establish a new method for the synthesis of D-prolinamide.Method D-proline was obtained from the asymmetric transformafion of L-proline via the formation of(S)-tartaric acid salt by using butanal as catalyst.Then,D-prolinamide was synthesized by amino protection,esterification,amidation and deprotection.Results and conclusion The yield of final product was 78.4% and optical purity was 99.3%.Comparing with patent synthetic procedure for D-prolinamide,it is a new synthetic procedure with better yield and purity and suitable for industrial manufacture. |
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| Keywords: | medicinal chemistry process improvement asymmetric synthesis chiral drug D-prolinamide |
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