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］。
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.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1995年第4期178-179,共2页
Chinese Journal of Pharmaceuticals
关键词
左氧氟沙星
苯并恶嗪
外消旋体拆分
中间体
levofloxacin,7,8-difluoro-3,4-dihydro-3-methy1-2H-[1,4] benzoxazine,optical resolution
