摘要
目的改进依帕司他的合成工艺。方法以3-羧甲基绕丹宁与α-甲基肉桂醛为起始原料,经碱催化下缩合、游离和精制制备得到依帕司他。结果依帕司他合成总收率83.5%,纯度99.87%。所得产品经熔点、质谱(MS)、核磁共振氢谱(^(1)H NMR)和核磁共振碳谱(^(13)C NMR)等方法确证。结论改进后的工艺稳定可靠、安全环保、产品纯度高、适宜工业化生产。
Objective To improve the synthesis process of epalrestat.Methods Starting from rhodanine-3-acetic acid andα-methyl cinnamaldehyde,epalrestat was obtained by condensation reaction catalyzed by base,acid neutralization and purification.Results The total yield of epalrestat reached 83.5%and the purity reached 99.87%.The structure of epalrestat was confirmed by melting point,MS,^(1)H NMR and ^(13)C NMR.Conclusion With safety,high purity and environmental protection,the improved process is stable,reliable and easy for the industrialization.
作者
颜世强
郭伟
何淑旺
曹焕英
解春文
王楚尧
YAN Shi-qiang;GUO Wei;HE Shu-wang;CAO Huan-ying;XIE Chun-wen;WANG Chu-yao(Shandong Dyne Marine Biopharmaceutical Co.,Ltd.,Weihai 264300,China)
出处
《食品与药品》
CAS
2022年第3期215-217,共3页
Food and Drug
基金
山东省自然科学基金重点项目(编号:ZR2020KH002)。
关键词
依帕司他
缩合
安全环保
工业化
epalrestat
condensation
safety and environmental protection
industrialization
