摘要
目的改进Enobosarm的合成工艺。方法以D-脯氨酸为起始物料,经缩合反应,溴内酯化反应,水解反应,缩合反应,取代反应生成Enobosarm。结果总收率由21.0%提高至51.4%,产物纯度99.8%,手性纯度99.8%。结论优化后的反应条件温和,工艺操作简便,适合工业化生产。
Objective To improve the synthesis process of Enobosarm.Methods Starting from D-proline,Enobosarm was obtained by condensation,bromolactonization,hydrolysis,condensation and substitution reactions.Results Through the improvement of synthesis process,the total yield increased from 21.0%to 51.4%,the product purity was 99.8%,and the chiral purity was 99.8%.Conclusion The optimized reaction conditions are mild,the process is simple and convenient,and is suitable for industrial production.
作者
邓玉晓
刘宜辉
樊志萍
任业明
段崇刚
孙晋瑞
DENG Yu-xiao;LIU Yi-hui;FAN Zhi-ping;REN Ye-ming;DUAN Chong-gang;SUN Jin-rui(Shandong Provincial Key Laboratory of Chemical Drugs,Shandong Academy of Pharmaceutical Sciences,Jinan 250101,China)
出处
《食品与药品》
CAS
2021年第2期138-141,共4页
Food and Drug
