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左氧氟沙星中间体苯并噁嗪的拆分
RESOLUTION OF LEVOFLOXACIN INTERMEDIATE 3,4-DIHYDROBENZOXAZINE
【摘要】 氧氟沙星的合成中间体苯并嗪[(±)1]先与(S)-N-对甲苯磺酰脯氨酰氯反应,经结晶分离,其母液(2a)水解后所得游离碱(1a)再与(1S)-(+)-10-樟脑磺酸成盐,重结晶后的盐(3)碱析得所需(S)-苯并嗪[(-)1]。
【Abstract】 Crystallization of the diastereoisomers [(+)2 and (-)2] formed from (± ) - 7, 8-difluoro-3, 4-dihydro-3-methy1-2H- [1, 4] -benzoxazine [ (±) 1] with (S)-N-(p-toluenesulfonyl) prolinyl chloude, there was obtained 2a [rich in (+)2]. Hydrolysis of 2a gave 1a [rich in (-) 1] which was resolved by(1s)-(+)camphor-10-sulfonic acid to afford the required (-) 1.
【关键词】 左氧氟沙星;
苯并噁嗪;
外消旋体拆分;
【Key words】 levofloxacin; 7; 8-difluoro-3; 4-dihydro-3-methy1-2H-[1; 4] benzoxazine; optical resolution;
【Key words】 levofloxacin; 7; 8-difluoro-3; 4-dihydro-3-methy1-2H-[1; 4] benzoxazine; optical resolution;
- 【文献出处】 中国医药工业杂志 ,CHINESE JOURNAL OF PHARMACEUTICALS , 编辑部邮箱 ,1995年04期
- 【分类号】R914
- 【被引频次】2
- 【下载频次】154