期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

抗癫痫药左乙拉西坦的工艺优化新方法

A Novel Method on the Process Optimization of Synthesizing Levetiracetam
在线阅读 下载PDF
导出
摘要 以(S)-α-乙基-氧代-1-吡咯烷乙酸为起始原料,在活化剂和氨气作用下,用两步一锅法制备左乙拉西坦。探讨了不同的活化剂、缚酸剂等因素对活性酯法成酰胺反应过程的影响,确定了最优物料投放比例;当以甲磺酰氯作为活化剂时,反应收率可达到约92.0%;改良后的工艺收率稳定,适合工厂工业化大规模生产。 Levetiracetam is prepared from （S）-alpha-ethyl-oxo-l-pyrrolidineacetic acid by the use of activating reagents and gaseous ammonia in one pot reaction. Bases on the influence of active ester method, the factors such as activating agents and bases were discussed, and then the optimal ratio of raw materials was determined. The yield can be about 92.0% using methane sulfonyl chloride as activating agent. The improved process is suitable for mass industrialized production.
作者 杨燕 周军全 姚跃良 吴范宏
机构地区 华东理工大学化学与分子工程学院 上海华理生物医药有限公司 上海应用技术学院
出处 《华东理工大学学报（自然科学版）》 CAS CSCD 北大核心 2013年第3期307-310,共4页 Journal of East China University of Science and Technology
关键词 左乙拉西坦 合成 工艺优化 levetiracetam synthesis process optimization
分类号 TQ463 [化学工程—制药化工]
  • 相关文献

参考文献11

  • 1Cossement E, MotteG, Geerts J P, etal. The preparation of ( S )-alpha-ethyl-2-oxo pyrrolidineacetamide: GB, 2225322 [P]. 1990.
  • 2Nash E M, Sangha K S. l.evetiracetam[J]. American Jour- nal of Health-System Pharmacy, 2001, 58(13):1195 1199.
  • 3Gualtieri F, Manetti D, Romanelli M N. Design and study of piracetam like noo tropices, controversial members of the problematic of congnition-enhancing drugs[J].Current Phar- maceutical Design, 2002, 8(2): 125-138.
  • 4Gobert J, Geerts J P, Dodson G. (S)-alpha-ethyl-2-oxo- 1-pyrrolidineacetamide compositions: US, 4837223 [P]. 1989.
  • 5Rizzuti Gianluigi, Gianolli Edoard. Synthesis of (S) alpha WO, 2006127300AI [P] 2006.
  • 6Gade Srinivas Reddy, Mallepalli Srinivas Reddy, Muvva Venkateshwarlu, et al. Processes for the preparation of Levetiracetam: WO, 2008077035A21[P]. 2008.
  • 7Corrado Colli, Massimiliano Forcato, Livius Cotarca. Process for the preparation oflevetiracetam: US, 7939676[P]. 2011.
  • 8Joseph Honore Lueien Michel Strubbe, Ruymond Armand Linz. New N substitutedlactams: GB, 1309692[P]. 1973.
  • 9AtesC, SurteesJ, Burteau AC, etal. Improved process for the preparation of (S)-alpha-ethyl-2-oxo-pyrrolidineacetamide and (R)-alpha-ethyl-2-oxo-pyrrolidineacetamide: CA, 02488325 [P]. 2004.
  • 10刘跃金,陈道鹏,梁良,刘丹,孙志祥.左乙拉西坦及其衍生物的合成[J].中国新药杂志,2007,16(11):860-864. 被引量：9

二级参考文献12

  • 1罗湘冀.左乙拉西坦的合成[J].药学进展,2004,28(9):413-417. 被引量：11
  • 2NICOLAUS BJR.Chemistry and pharmacology of nootropies[J].Drug Develop Res,1992,2(5):463-464.
  • 3UCB Societe Anonyme.(S)-alpha-ethyl-2-oxo-1-pyrrolidine acetamide:USP,4,696,943[P].1985-05-14.
  • 4UCB Societe Anonyme.Pharmacologically active N-substituted lactams:Belgium Patent,762728[P].1971-08-10.
  • 5MACHIDA M,OYADOMARI S,TAKECHI H,et al.Photocyclization of succinimide derivatives with amido group in side chains synthesis of tricyclie pyrrolo[1,2-a]pyrazine ring systems[J].Heterocycles,1982,19(11):2057-2060.
  • 6GUDASHEVA TA,OSTROVSKAYS RU,TROFIMOV SS,et al.Peptide analogs of piracetam as ligands of putative nootropic receptors[J].Khim Farm Zh,1985,19(11):1322-1329.
  • 7HASKEL TH,HUTT MP JR,NICOLAIDES ED.Antibacterial amide compounds:US Patent,4,267,180[P].1981-05-12.
  • 8CALLARDO CARRERA A.Pyrolidineacetamides:Spanish Patent,ES537951[P].1985-11-01.
  • 9FUJIMAKI Y,HASHIMOTO K,SUDO K,et al.Biotransformation of a new pyrrolidinone cognition-enhancing agent:isolation and identification of metabolites in human urine[J].Xenobiotica,1990,20(10):1080-1094.
  • 10张万金,王尔华.α-乙基-[(2-氧)-1-]吡咯烷乙酰胺衍生物的合成[J].广东药学院学报,2000,16(4):263-264. 被引量：3

共引文献8

华东理工大学学报（自然科学版）
2013年 第3期

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部