维格列汀的合成路线改进

发布时间：2018-10-31 13:04

【摘要】：目的:改进维格列汀的合成路线。方法:以L-脯氨酸为起始原料,经Boc保护、酰胺化、脱水、脱保护成盐、N-氯乙酰化得(S)-1-(2-氯乙酰基)-2-氰基吡咯烷(2),最后与3-氨基-1-金刚烷醇缩合即得目标产物维格列汀。结果:目标化合物的结构经质谱(ESI-MS)、核磁共振氢谱、碳谱(1H-NMR,13C-NMR)等确证,总收率32%,产品纯度99.8%以上。结论:改进后的工艺操作简单,产率较高,产品纯度高,适合工业化生产。
[Abstract]:Objective: to improve the synthetic route of Viaglline. Methods: (S) 1- (2-chloroacetyl) -2-cyanopyrrolidine (2) was synthesized from L-proline by Boc protection, amidation, dehydration, deprotection and N-chloroacetylation. Finally, the target product was obtained by condensation with 3-amino-1-adamantanol. Results: the structure of the target compound was confirmed by mass spectrometry (ESI-MS), nuclear magnetic resonance (NMR) and carbon spectrum (1H-NMR-13C-NMR). The total yield was 32 and the purity of the product was over 99.8%. Conclusion: the improved process has the advantages of simple operation, high yield and high purity. It is suitable for industrial production.
【作者单位】：河北科技大学化学与制药工程学院;河北省药用分子化学重点实验室-省部共建国家重点实验室培育基地;
【分类号】：R914.5

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