【摘要】：目的:改進(jìn)維格列汀的合成路線。方法:以L-脯氨酸為起始原料,經(jīng)Boc保護(hù)、酰胺化、脫水、脫保護(hù)成鹽、N-氯乙酰化得(S)-1-(2-氯乙�；�)-2-氰基吡咯烷(2),最后與3-氨基-1-金剛烷醇縮合即得目標(biāo)產(chǎn)物維格列汀。結(jié)果:目標(biāo)化合物的結(jié)構(gòu)經(jīng)質(zhì)譜(ESI-MS)、核磁共振氫譜、碳譜(1H-NMR,13C-NMR)等確證,總收率32%,產(chǎn)品純度99.8%以上。結(jié)論:改進(jìn)后的工藝操作簡單,產(chǎn)率較高,產(chǎn)品純度高,適合工業(yè)化生產(chǎn)。
[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.
【作者單位】： 河北科技大學(xué)化學(xué)與制藥工程學(xué)院;河北省藥用分子化學(xué)重點(diǎn)實(shí)驗(yàn)室-省部共建國家重點(diǎn)實(shí)驗(yàn)室培育基地;
【分類號】：R914.5

【參考文獻(xiàn)】

相關(guān)期刊論文 前1條

1 樊新星;徐s，

本文編號：2302291