摘要
目的研究dl-麻黄碱的化学拆分策略。方法根据非对映异构体在溶剂中溶解度的不同进行拆分。结果与结论利用拆分试剂L-(-)-二苯甲酰基酒石酸可将dl-麻黄碱同时拆分为D-(-)-麻黄碱和L-(+)-麻黄碱,拆分收率可达80%以上,ee%值可达99%以上,拆分试剂L-(-)-二苯甲酰基酒石酸的回收率达96.3%。该法有望用于工业化大规模生产光学纯的D-(-)-麻黄碱和L-(+)-麻黄碱。
Aim To obtain optically pure D-( - )-ephedrine and L-( + )-ephedrine. Methods To resolve dl- ephedrine according to solubility difference of diastereoisomers formed by D-( - )-ephedrine and L-( + )- ephedrine with resolving agent. Results and conclusion L-( - )-dibenzoyltartaric acid was used to resolve dl-ephedrine to get optically pure isomers with the resolution yield of more than 80 %. The values of ee% of D-( - )-ephedrine and L-( + )-ephedrine are more than 99 %. L-( - )-dibenzoyltartaric acid could be recovered with the yield of 96 % or so. The method reported here has a great promise for producing optically pure D-( - )-ephedrine and L-( + )-ephedrine in large scale.
出处
《中国药物化学杂志》
CAS
CSCD
2008年第3期195-199,共5页
Chinese Journal of Medicinal Chemistry