期刊文献+

抗肿瘤药物泊马度胺的合成工艺改进 被引量:1

Improved Sythesis of Antitumor Agent Pomalidomide
下载PDF
导出
摘要 改进抗肿瘤药泊马度胺的合成工艺,以3-硝基邻苯二甲酸为原料,合成3-硝基邻苯二甲酸酐;再与谷氨酰胺反应,经氨解、缩合、还原得到目标产物泊马度胺,反应总收率60.8%。 This study is to optimize production of antitumor agent pomalidomide. The 3-nitrophthalic anhydride was synthesized from 3-nitrophthalic acid and then reacted with glutamine, and the final product pomaliddomide was synthesized by ammonolysis, condensation and reduction. The total yield is 60.8%.
出处 《药学与临床研究》 2016年第3期242-243,共2页 Pharmaceutical and Clinical Research
基金 国家自然科学基金项目(81473692)
关键词 泊马度胺 工艺改进 合成 Pomaliddomide Process optimization Synthesis
  • 相关文献

参考文献8

二级参考文献91

  • 1袁修华,郭海泉,邱雪鹏,康传清,刘旭东,高连勋.一步法合成沙利度胺及其重要的衍生物[J].高等学校化学学报,2005,26(8):1477-1479. 被引量:5
  • 2Tricot S, Berthon C, Venon M, et al. Thalidomide in multiple myeloma in the elderly [J]. Aging Health, 2009, 5 (1) : 1-17.
  • 3Galustian C, Meyer B, Labarthe M, et al. The anticancer agents lenalidomide and pomalidomide inhibit the proliferation and function of T regulatory cells [J]. Cancer Immunology Immunotherapy, 2009, 58 (7) : 1033-1045.
  • 4Zhu D, Corral GL, Fleming YW, et al. Immunomodulatory drugs Revlimid (lenalidomide) and CC-4047 induce apoptosis of both hematological and solid tumor cells through NK cell activation [J]. Cancer Immunology Immunotherapy, 2008, 57 (12) : 1849-1859.
  • 5Muller GW, Saindane MT, Chuansheng GE, et al. Processes for the preparation of 4-amino-2- (2,6-dioxopiperidin-3- yl) isoindoline-l,3-dione: EP, 20060786385 [P]. 2006-06-29.
  • 6Zhu XX, Giordano T, Yu QS, et al. Thiothalidomides: novel isosteric analogues of thalidomide with enhanced TNF-α inhibitory activity [J]. J Med Chem, 2003, 46 (24) : 5222-5229.
  • 7Perino S, Contino-Pepin C, Satchi-Fainaro R, et al. Inhibition of angiogenesis by THAM-derived cotelomers endowed with thalidomide moieties [J]. Bioorg Med Chem Lett, 2004, 14 (2) : 421-425.
  • 8Stewart SG, Spagnolo D, Polomska ME, et al. Synthesis and TNF expression inhibitory properties of new thalidomide analogues derived via Heck cross coupling [J]. Bioorg Med Chem Lett, 2007, 17 (21) : 5819-5824.
  • 9Varala R, Adapa SR. A practical and efficient synthesis of thalidomide via Na/liquid NH3 methodologyl [J].Org Process Res Dev, 2005, 9 (6) : 853-856.
  • 10Yuan L H, Feng W, Yamato K, et al. Highly effi- cient, one-step macrocyclizations assisted by the folding and preorganization of precursor oligomers [ J ]. J Am Chem Soc,2004,126 : 11120 - 11121.

共引文献29

同被引文献5

引证文献1

二级引证文献3

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