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

盐酸噻加宾的合成 被引量：1

Synthesis of Tiagabine Hydrochloride
下载PDF
导出
摘要 2-溴-3-甲基噻吩的格氏试剂与氯甲酸甲酯加成后“一锅”与环丙基溴化镁加成制得环丙基二(3-甲基-2-噻吩基)-甲醇,开环后与(R)-(-)-3-哌啶甲酸乙酯经缩合、水解和成盐反应制得盐酸噻加宾,总收率41%。 Tiagabine hydrochloride was synthesized from 2-bromo-3-methylthiophene Grignard reagent by tandem addition with methyl chloroformate and cyclopropylmagnesium bromide to give cyclopropyl-bis （3-methylthiophen-2-yl） - methanol, which underwent ring opening and condensed with ethyl （R） - （一） -piperidine-3-carboxylate, hydrolysis and HCl salt formation in 41% overall yield.
作者 赵学清 李飞 刘秀兰
机构地区 福建省微生物研究所 南京中医药大学药学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2006年第2期75-77,共3页 Chinese Journal of Pharmaceuticals
基金 福建省青年科技人才创新基金(2004J078)
关键词 噻加宾 GABA摄取抑制剂 抗癫痫药 合成 tiagabine GABA uptake inhibitor antiepileptic synthesis
分类号 R971.6 [医药卫生—药品]
  • 相关文献

参考文献4

  • 1叶金朝.癫痫治疗药　噻加宾(Tiagabine)[J].国外医药（合成药．生化药．制剂分册）,1999,20(2):84-85. 被引量：2
  • 2Kaelviaeinen R. Long-term safety of tiagabine [J]. Epilepsia,2001, 42 (Suppl. 3) : 46-48.
  • 3Andersen KE, Braestrup C, Gronwald FC, et al. Synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R) - 1- [4,4-bis-(3-methyl-2-thienyl) -3-butenyl]-3-piperidinecarboxylic acid(Tiagabine) as an anticonvulsant drug candidate [J]. J Med Chem, 1993, 36(12):1716-1725.
  • 4Ahrndt P, Petersen HB, Chang VH, et al. Modification form of the R- (-) -N- [4,4-di (3-mehtylthien-2-yl) but-3-enyl] nipecotic acid hydrochloride [P]. US: 5958951, 1999-09-28,WO: 9747619, 1997-12-18. (CA 1998, 128: 80001).

共引文献1

同被引文献8

  • 1The UK drug information pharmacists group.New medicineon the market-Tiagabine. . 1999
  • 2Jenkins.Nutritional characteristics of alkali-treated protein. Journal of Agricultural and Food Chemistry . 1984
  • 3OM Larsson,GAR Johnston,A Schousboe.Differences in uptake kinetics of cis-3-aminocyclohexane carboxylic acid into neurons and astrocytes in primary cultures. Brain Research . 1983
  • 4KaelviaeinenR.Long-termsafetyoftiagabine. Epilepsia . 2001
  • 5Masters,PM,Friedman,MJ.Racemization of amino acids in alkali-treated food proteins. Journal of Agricultural and Food Chemistry . 1979
  • 6Liardon,R,Hurrell,RF.Amino acid racemization in heated and alkali-treated proteins. Journal of Agricultural and Food Chemistry . 1983
  • 7Larsson,OM,Krogsgaard-Larsen,P,Schousboe,A.Characterization of the uptake of GABA, nipecotic acid and cis-4-OH-nipecotic acid in cultured neurons and astrocytes. Neurochemistry International . 1985
  • 8Andersen,K. E.,Braestrup,C.,Gronwald,F. C.,Jorgensen,A. S.,Nielsen,E. B.,Sonnewald,U.,Sorensen,P. O.,Suzdak,P. D.,Knutsen,L. J.The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure–activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate. Journal of Medicinal Chemistry . 1993

引证文献1

中国医药工业杂志
2006年 第2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