唐顺之1,2,3,骆征山1,2,3,邓奉坚1,2,3,李松涛1,2,3,文舒琪1,2,3, 彭万才1,2,3,牟肖男1,2,3,许文东1,2,3.半合成法制备二硬脂酰磷脂酰乙醇胺[J].中国油脂,2025,50(11):.[TANG Shunzhi1,2,3, LUO Zhengshan1,2,3, DENG Fengjian1,2,3, LI Songtao1,2,3, WEN Shuqi1,2,3, PENG Wancai1,2,3, MU Xiaonan1,2,3, XU Wendong1,2,3.Preparation of distearoylphosphatidylethanolamine by semi-synthesis method[J].China Oils and Fats,2025,50(11):.]
半合成法制备二硬脂酰磷脂酰乙醇胺
Preparation of distearoylphosphatidylethanolamine by semi-synthesis method
       出版日期:2025-11-20
DOI:10.19902/j.cnki.zgyz.1003-7969.240627
中文关键词:  半合成法  蛋黄卵磷脂  二硬脂酰磷脂酰乙醇胺  合成磷脂
英文关键词:semi-synthesis method  egg yolk lecithin  distearoylphosphatidylethanolamine  synthetic phospholipid
基金项目:广东省科技计划项目广东省药用脂质重点实验室(2023B1212070030)
作者单位
唐顺之1,2,3,骆征山1,2,3,邓奉坚1,2,3,李松涛1,2,3,文舒琪1,2,3, 彭万才1,2,3,牟肖男1,2,3,许文东1,2,3 1.广州白云山汉方现代药业有限公司,广州 510240 2.中药制药过程技术与新药创制国家工程研究中心, 广州 510240 3.广东省药用脂质重点实验室,广州 510240 
Author NameAffiliation
TANG Shunzhi1,2,3, LUO Zhengshan1,2,3, DENG Fengjian1,2,3, LI Songtao1,2,3, WEN Shuqi1,2,3, PENG Wancai1,2,3, MU Xiaonan1,2,3, XU Wendong1,2,3 1.Guangzhou Baiyunshan Hanfang Modern Pharmaceutical Co. , Ltd. , Guangzhou 510240, China
2.National Engineering Research Center for Pharmaceutical Process Technology and New Drug Development of Traditional Chinese Medicine, Guangzhou 510240, China
3.Guangdong Provincial Key Laboratory of Medicinal Lipids, Guangzhou 510240, China 
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中文摘要:
      旨在为二硬脂酰磷脂酰乙醇胺(DSPE)的制备和蛋黄卵磷脂产业深加工提供新思路,探究了半合成法制备DSPE的可行性。以蛋黄卵磷脂中提取的磷脂混合物为原料,优化醇解、酯化、柱层析等反应条件,并进行放大实验。结果表明:半合成法制备DSPE的最佳反应条件为醇解反应的强碱为甲醇钠、强碱用量为0.3倍量(以中间体混合物Ⅰ质量计),酯化反应的缩合剂为二环己基碳二亚胺、催化剂为4-二甲氨基吡啶,柱层析所用洗脱剂中的短链醇为甲醇、硅胶柱与填料的径高比为1∶ 6。在最佳反应条件下对该工艺进行10倍放大验证,DSPE收率为18.2%。经高效液相色谱检测,DSPE产品纯度为99.8%。综上,采用半合成法制备DSPE是可行的。
英文摘要:
      In order to provide new ideas for the preparation of distearoylphosphatidylethanolamine (DSPE) and deep processing of egg yolk lecithin, the feasibility of preparing DSPE by semi-synthesis method was explored. The phospholipid mixture extracted from egg yolk lecithin was used as raw material to optimize the reaction conditions such as alcoholysis, esterification and column chromatography, and the amplification experiment was carried out. The results showed that the optimal reaction conditions for the synthesis of DSPE were as follows: the strong base of alcoholysis reaction was sodium methoxide, the amount of strong base was 0.3 times (based on the mass of intermediate mixture Ⅰ), the condensation agent of esterification reaction was dicyclohexylcarbodiimide (DCC), the catalyst was 4-dimethylaminopyridine (DMAP), the short-chain alcohol in the eluent used in column chromatography was methanol, and the diameter-height ratio of silica gel column to filler was 1∶ 6. The process was validated at lotimes amplification, and the yield of DSPE was 18.2% under the optimum reaction conditions. The purity of DSPE was 99.8% as determined by high performance liquid chromatography. In summary, preparation of DSPE by semi-synthesis method is feasible.
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