期刊文献+

1-芳基-2-吡咯烷酮衍生物的合成研究

Study on the Synthesis of 1-Aryl-2-pyrrolidinone Derivatives
下载PDF
导出
摘要 1-芳基-2-吡咯烷酮衍生物是重要的有机合成中间体。以苯佐卡因为原料,经溴代、缩合、环合合成了目标产物,产物总收率达72.25%。其结构经1H NMR,MS进行了确证。该方法具有操作简便、成本低、收率高等优点。 1-Aryl-2-pyrrolidinone derivatives are important intermediates for organic synthesis.A novel process was developed for the synthesis of the title compound in an overall yield of 72.2% starting from benzocaine via bromination,nucleophilic substitution and cyclization.The structure of the target compound was confirmed with 1H NMR and MS.This method shows advantages of easy operation,low cost and high yield.
出处 《精细化工中间体》 CAS 2012年第6期39-41,44,共4页 Fine Chemical Intermediates
关键词 1-芳基-2-吡咯烷酮 丙烯酸乙酯 合成 pyrrolidinone ethyl acrylate synthesis
  • 相关文献

参考文献12

  • 1Susumu K. 3-Benzylidene-1-carbamoyl-2-pyrrolidone compounds useful as anti-inflammatory agents[P].US,5319099,1994.
  • 2Zhuang C L,Miao Z Y,Zhu L J. Discovery.synthesis,and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein Interaction[J].Journal of Medicinal Chemistry,2012.9630-9642.
  • 3Kazmierski W M,Andrews W,Furfine E. Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties[J].Bioorganic and Medicinal Chemistry Letters,2004,(22):5689-5692.
  • 4张万金,王尔华.促智药奈非西坦的合成[J].化工时刊,2005,19(3):14-15. 被引量:2
  • 5Brouillette W J,Atigadda V R,Duarte F. Potent Inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent[J].Journal of Medicinal Chemistry,1999.2332-2343.
  • 6Brouillette W J,Bajpai S N,Ali S M. Pyrrolidinobenzoic Acid Inhibitors of Influenza Virus Neuraminidase:Modifications of Essential Pyrrolidinone Ring Substituents[J].Bioorganic and Medicinal Chemistry Letters,2003.2739-2749.
  • 7Tran J A,Tucci F C,Arellano M. Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands[J].Bioorganic and Medicinal Chemistry Letters,2008.1931-1938.
  • 8Qiao J X,Chang C H,Cheney D L. SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa[J].Bioorganic and Medicinal Chemistry Letters,2007.4419-4427.
  • 9布伦德尔.取代的吡咯烷-2-酮、哌啶-2-酮和异噻唑烷-1,1-二氧化物、它们作为Kv1.5钾通道阻断剂的用途和包含它们的药物制剂5钾通道阻断剂的用途和包含它们的药物制剂[P].中国,2006800225732008.
  • 10Wu Y H. Pyrrolidines.I.1-Substituted 3-Pyrrolidinylmethyl Alcohols and Chlorides[J].Tetrahedron,1961.1519-1524.

二级参考文献20

  • 1周斌.益智药 富马酸尼拉西坦[J].国外医药(合成药.生化药.制剂分册),1994,15(3):172-173. 被引量:3
  • 2虞心红,王建兵,吕和平,李晓勇,傅收,王伟,陆丁,沈永嘉.富马酸奈拉西坦的合成工艺研究[J].中国药物化学杂志,2005,15(4):237-240. 被引量:4
  • 3金永寿.奈非西坦改善脑功能障碍的作用[J].国外医药(合成药.生化药.制剂分册),1996,17(2):98-101. 被引量:9
  • 4方正,杨照,徐芳.富马酸奈拉西坦的合成[J].中国医药工业杂志,2006,37(6):375-376. 被引量:3
  • 5GB 2 053 909A. UK Patent Application[S].
  • 6CN 1 085 893[S].
  • 7Shizuo Kitahala.Colored microsphere-containing dispersion compositions[P].JP:15 17 694,1993-01-26.
  • 8Shizuo Kitahala,Hiroyuki Watanabe,Takuji Kishimoto, et al.Fuel oils containg azomethinium salts for improved dispersibility of particulate materials[P].US:5 294 233,1994-03-14.
  • 9NaKamura Masao,Takagishi Yukio,Inagaki Katsumi.Rubber composition with good exotherm resistance,tensile strength,workability,and antistatic properties[P].JP:97 39 055,1997-10-23.
  • 10Rajadhyaksha Vithal J.Plant pest control[P].EP:77 078,1983-04-20.

共引文献17

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