期刊文献+

5-甲氧基-2-环丙胺基嘧啶的合成研究

Synthesis of N-cyclopropyl-5-methoxypyrimidin-2-amine
原文传递
导出
摘要 研究了一种以2,4-二氯-5-甲氧基嘧啶、环丙胺为起始原料,经脱氯、钯催化交叉偶联二步反应合成新型有机医药中间体5-甲氧基-2-环丙胺基嘧啶的工艺,总收率约为63%。分析探讨了反应机理和影响因素,产品结构经~1H NMR、MS表征确认。 Found a synthesis process of N-cyclopropyl-5-methoxypyrimidin-2-amine(a new organic pharmaceutical intermediates) with the original material of 2,4-dichloro-5-oxo-methylpyrimidine and eyclopropylamine through two steps of chemical reaction by dechlorination and palladium-catalyzed cross-coupling. Total yield of the reaction is 63 %. Reaction mechanism and the impact factors were discussed. The structure of the products were characterized by 1H NMR. MS spectra.
出处 《计算机与应用化学》 CAS 2015年第5期572-574,共3页 Computers and Applied Chemistry
基金 杭州市属高校绿色精细化工研究与技术转化重点实验室资助项目(HZJ2012-02)
关键词 5-甲氧基-2-环丙胺基嘧啶 钯催化 交叉偶联 合成 N-cyelopropyl-5-methoxypyrimidin-2-amine Palladium-catalyzed cross-coupling synthesis process
  • 相关文献

参考文献13

  • 1Bakavoli M, Bagherzadeh G Vaseghifar M, et al. Molecular iodine promoted synthesis of new pyrazolo[3, 4-d] pyrimidine derivatives as potential antibacterial agents. Eur J Med Chem, 2010, 45(2): 647-650.
  • 2Khobragade C N, Bodade R G, Konda S O, et al. Synthesis and antimierobial activity of novel pyrazolo[3, 4-d] pyrimldine derivatives. Eur J Med Chem, 2010, 45(4):1635-1638.
  • 3Yewale S B, Ganorkar S B, Baheti K G, et al. Novel 3 -substituted- 1 -aryl-5 -phenyl-6-anilinopyrazolo [3, 4-d] pyrimidin-4-ones: Docking, synthesis and pharmacological evaluation as a potential anti - inflammatory agents. Bioorg Med Chem Lett, 2012, 22(21):6616-6620.
  • 4Rashad A E, Hegab M I, Abdel-Megeid R E, et al. Synthesis and antiviral evaluation of some new pyrazole and fused pyrazolopyrimidine derivatives. Bioorg Med Chem, 2008, 16(15):7102-7106.
  • 5Kimura Makoto, Kuwano Seiichi, Sawaki Yasuhiko, et al. New 9-tluorene- type trisprocyellc compounds tor thermally stalgle hole transport materials in OLEDs. Journal of Materials Chemistry, 2005, 15(24):2393- 2398.
  • 6Klaus S, Neumann H, Zapf A, et al. A general and efficient method for the formulation of aryl and vinyl halides. Angew Chem Int Ed, 2006, 45:154-158.
  • 7Liang B, Huang M W, You Z J,et al. Pal-catalyzed copper-free carbonylative sonogashira reaction of aryl iodides with alkynes for the synthesis of alkynyl ketones and flavones by using water as a solvent. J Org Chem, 2005, 70:6097-6100.
  • 8Wu X Y, Larhed M. Microwave-enhanced amino earbonylations in water. Org Lett, 2005, 7 (15):3327-3329.
  • 9李淼,刘若霖,李志念,刘长令,李正名.新型含嘧啶环的甲氧基丙烯酸酯类化合物的设计、合成及杀菌活性[J].农药,2009,48(6):405-408. 被引量:8
  • 10商琳琳,贾云宏,蔡东.5-二乙氨甲基-6-甲基-2,4-二羟基嘧啶的合成及抗炎活性[J].化学世界,2010,51(6):355-358. 被引量:2

二级参考文献68

  • 1庞素华,綦聚鳌,吴冬梅,张清德.嘧啶衍生物的Mannich碱合成[J].化学试剂,1994,16(3):178-180. 被引量:3
  • 2尚尔才,刘长令,杜英娟.嘧啶类农药的研究进展[J].化工进展,1995,14(5):8-15. 被引量:24
  • 3柏亚罗.Strobilurins类杀菌剂研究开发进展[J].农药,2007,46(5):289-295. 被引量:72
  • 4刘长令,李林,张弘,等.取代唑类化合物及其制备与应用[P].CN1657524,2004-02-20.
  • 5RINGOM R,AXEN E,UPPENBERG J,et al.Substituted Benzylamino-6-(trifluoromethyl)pyrimidin-4(IH)-ones:A Novel Class of Selective Human A-FABP Inhibitors[J].Bioorg Med Chem,2004,14(17):4449-4452.
  • 6LIU Chang-ling,CHAI Bao-shan,ZHANG Hong,et al.Substituted Pyrimidine Ether Compounds and Uses Thereof:WO,2008145052[P].2008-12-04.
  • 7LIU Chang-ling,LI Lin,LI Zheng-ming.Design,Synthesis,and Biological Activity of Novel 4-(3,4-Dimethoxyphenyl)-2-methylthiazole-5-carboxylic Acid Derivatives[J].Bioorg Med Chem,2004,14(12):2825-2830.
  • 8薛伟,王献友,宋宝安,金林红,胡德禹,杨松.嘧啶类化合物杀菌活性研究进展[J].农药,2007,46(8):505-509. 被引量:19
  • 9Muci A R, Buchwald S L. Top Curr Chem, 2002, 219: 131.
  • 10Kantchev E A B, O'Brien C J, Organ M G. Angew Chem, Int Ed, 2007, 46: 2768.

共引文献10

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