摘要
目的制备右旋佐匹克隆。方法以2,3-吡嗪二酸酐和2-氨基-5-氯吡啶为起始原料,经酯化、环合、不对称还原、成酯和精制反应得到右旋佐匹克隆。结果与结论目标化合物的结构经1H-NMR谱确证。新合成方法操作简便、收率高,适合工业化生产。产品光学纯度大于99.9%,化学纯度大于99.5%。
This paper improved the synthesis of eszopiclone. At present, the preparation methods of eszopiclone is zopiclone racemic resolution. However, the zopiclone racemic resolution is limited industrially due to its high cost and low yield. The aim of this study is to propose a modified asymmetric reduction method to prepare eszopiclone for industrialized production. 2,3-Pyrazine anhydride and 2-amino-5-chloropyridine were used as the starting materials by condensation, cyclization, asymmetric reduction, condensation and purification reaction to obtain eszopiclone. The （ R ） -3,3-diphenyl-1 -methylpyrrolidino [ 1,2-c ] -1,3,2-oxazaborole was used as the catalyst. The BH3-THF was used as reducing agent. The total yield of the eszopiclone was 44.0%.
出处
《中国药物化学杂志》
CAS
CSCD
2014年第5期387-389,共3页
Chinese Journal of Medicinal Chemistry
