摘要
利用外消旋体在溶液中溶解度相互竞争的特点,在使用结晶法拆分消旋佐匹克隆时,加入少量的右佐匹克隆或其苹果酸盐,通过与D-苹果酸成盐、冷却结晶的方法,可以简便有效地拆分出右佐匹克隆D-苹果酸盐,再经过中和、萃取、浓缩、结晶,即可得到右佐匹克隆。通过控制加入的右佐匹克隆或其苹果酸盐的量,得到了光学纯度(ee)大于99.9%的右佐匹克隆,且其收率在35%以上。
The solubilities of racemates in solution compete with each other, thus, adding a small amount of eszopiclone or eszopiclone D-malate to zopiclone, the eszopiclone D-malate can be easily and effectively obtained by reacting with D-malate, cooling, and crystallization. Then, eszopiclone can be got through neutralization, extraction,concentration, and crystallization. By controlling the amount of added eszopiclone or eszopiclone D-malate, the eszopiclone with an enantiomeric purity greater than 99% was prepared, and the yield was over 35%.
作者
傅麟勇
郭圣荣
FU Linyong;GUO Shengrong
出处
《上海化工》
CAS
2018年第1期26-29,共4页
Shanghai Chemical Industry
关键词
佐匹克隆
右佐匹克隆
D-苹果酸
拆分
结晶
Zopiclone
Eszopiclone
D-malic acid
Chiral separation
Crystallization
