L-α-甘油磷酸胆碱合成工艺的改进

发布时间：2018-06-25 05:59

本文选题：甘油磷酸胆碱 + 阿尔茨海默病　；参考：《中国新药杂志》2015年04期

【摘要】：目的:改进L-α-甘油磷酸胆碱(L-α-GPC)的合成工艺,提高合成收率。方法:以D-甘露糖醇为原料,经缩酮化、氧化、还原制得D-亚异丙基甘油,再与2-氯-2-氧-1,3,2-环氧磷戊烷进行酯化反应,然后用三甲胺进行氨化,最后水解除去丙叉基得目标化合物L-α-甘油磷酸胆碱(L-α-GPC)。结果:总收率从9.5%提高到38.6%(以D-甘露糖醇计),目标化合物的结构经元素分析,IR,1HNMR,13C-NMR和MS谱等确证。结论:通过对L-α-甘油磷酸胆碱的合成的改进,把传统的软磷脂水解提取工艺用化学合成法来代替,提高了收率,降低了成本,适合工业化生产。
[Abstract]:Objective: to improve the synthesis process of L-伪-glycerophosphate choline (L-伪 -GPC) and improve the yield. Methods: D- isopropyl glycerol was synthesized from D- mannol by Ketal reaction, oxidation and reduction. D- isopropyl glycerol was synthesized by esterification with 2-chloro-2-oxo-3-trioxy-3-epoxyphosphopentane, and then aminated with trimethylamine. Finally, the target compound L- 伪 -glycerophosphate choline (L- 伪 -GPC) was obtained by hydrolysis. Results: the total yield was increased from 9.5% to 38.6% (based on D-mannol). The structure of the target compound was confirmed by elemental analysis, IR 1H N MRN 13C-NMR and MS spectra. Conclusion: by improving the synthesis of L- 伪 -glycerophosphate choline, the traditional hydrolysis and extraction process of soft phospholipid is replaced by chemical synthesis method, which improves the yield, reduces the cost and is suitable for industrial production.
【作者单位】：北京双鹭药业股份有限公司;北京嘉林药业有限公司;
【分类号】：R914.5

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