| 消旋棉酚拆分的研究——Ⅱ.手性α-甲基苯乙胺及α-甲基苄胺为拆分剂 |
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| 引用本文： | 郑多楷,司伊康,孟佳克,黄量.消旋棉酚拆分的研究——Ⅱ.手性α-甲基苯乙胺及α-甲基苄胺为拆分剂[J].药学学报,1990,25(6):417-422. |
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| 作者姓名： | 郑多楷 司伊康 孟佳克 黄量 |
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| 作者单位： | 中国医学科学院药物研究所,北京100050 |
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| 摘 要： | 本文报道用中压柱色谱快速分离S或R-α-甲基苯乙胺及S或R-α-甲基苄胺缩(±)-棉酚的方法,可得光学活性胺缩(+)或(一)-棉酚非对映体,经水解分别得到(+)或(一)-棉酚。并证明胺缩光学活性棉酚非对映体之间有互相转化的性质,此特性可利用于棉酚对映体的转化。
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| 关 键 词： | 棉酚 α-甲基苯乙胺 α-甲基苄胺 (+)和(-)-棉酚 消旋反应 |
| 收稿时间： | 1989-10-06 |
Studies on the resolution of racemic gossypol. II. By chiral alpha-methylphenethylamine and alpha-methylbenzylamine |
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| DK Zheng,YK Si,JK Meng and L Huang.Studies on the resolution of racemic gossypol. II. By chiral alpha-methylphenethylamine and alpha-methylbenzylamine[J].Acta Pharmaceutica Sinica,1990,25(6):417-422. |
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| Authors: | DK Zheng YK Si JK Meng and L Huang |
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| Institution: | Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing. |
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| Abstract: | A simplified and more practical method for the resolution of racemic gossypol was developed by quick chromatographing the condensation products of either (S) or (R)-alpha-methylphenethylamine and alpha-methylbenzylamine with racemic gossypol on a silica column using diethylether/light petroleum as eluent. The optically active gossypol thus obtained showed specific rotation alpha]D of (+) or (-)370 +/- 10 degrees, with ee% 96.8 and 98.8 respectively and chemical purity greater than 99% by HPLC. Isomerization of the amino condensates of optically active gossypol through the racemization of the binaphthalene moiety of gossypol was observed, though gossypol itself is optically stable in such condition. The rate of racemization varied with the structure of the amine moiety and solvent present and was increased by light and free radical initiator. |
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| Keywords: | α- Methylphenethylamine α-M ethylbenzylamine (+)and (-) -gossypol Racemization Gossypol |
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