期刊文献+

比卡鲁胺的合成工艺改进 被引量:1

Improvement on Synthetic Process of Bicalutamide
下载PDF
导出
摘要 以甲基丙烯酰氯为原料,经N-酰化、环氧化、缩合和氧化合成了比卡鲁胺,总收率为57.6%,纯度为98.3%,并通过~1 HNMR、MS对其结构进行了确认。 Using methacryloyl chloride as a raw material,bicalutamide with the overall yield of 57.6% and the purity of 98.3% was synthesized by a four-step reaction of N-acylation,epoxidation,condensation and oxidation. The structure of bicalutamide prepared was confirmed by 1 HNMR and MS.
出处 《化学与生物工程》 CAS 2017年第4期39-41,46,共4页 Chemistry & Bioengineering
基金 湖北省自然科学基金重点项目(2011CDA048) 武汉工程大学研究生创新基金资助项目(CX2015074)
关键词 比卡鲁胺 药物合成 工艺改进 hicalutamide drug synthesis process improvement
  • 相关文献

参考文献6

二级参考文献32

  • 1刘雅茹,冯雪松,孟繁浩,刘俊亭.抗雄激素药物比卡鲁胺的合成[J].中国医科大学学报,2005,34(6):518-519. 被引量:8
  • 2Richard J.Thurlow. Treatment Options for Benign Prostatic Hyperplasia[J]. Emerging Drugs, 1998, 3 (1) :225- 246.
  • 3Laura Sepp-Lorenzino, Susan Slovin. Prostate Cancer:Therapeutic Patent Review [J ]. Exp. Opin.Ther Patents, 2000,10(12) :1833-1842.
  • 4Ekwuribe Nnochiri N,James Kenneth D. Resolution of Intermediates in the Synthesis of Substantially Pure Bicalutamide[P]. WO 01-34 563 A1,2001.
  • 5Howard Tucker, Crook J W, Chesterson G J, Nonsteroidal Antiandrogens. Synthesis and Structure-Activity Relationships of 3-Substituted Derivatives of 2-Hydroxypropionanilides [J]. J. Med. Chem., 1988, 31:954-959.
  • 6Howard Tucker,Macclesfield. Amide Derivatives[P].4 636 505,1987.
  • 7Winston Ho,Gene F Tutwiler,Sandra C Cottrell,Dava J. Morgans. Alkylglycidic Acidz Potential New Hypoglycemic Agents[J].J. Med. Chem.,1986,29:2184-2190.
  • 8Mebee ET,Lowery OR.Some dihalo-(trifluoromethyl)-benzenes[J]. J Am Chem Soc, 1951,73:3932.
  • 9Edwards JP,West SJ,Pooley CL, et al. New nonsteroidalandrogen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone[J].Bioorg Med Chem Lett, 1998,8(7):745.
  • 10Howard T,Crook JW,Chesterson GJ.Nonsteroidal antiandrogens.Synthesis and structure activity relationships of 2-hydroxypropionanilides[J].Med Chem,1988,31 (5):954-959.

共引文献13

同被引文献1

引证文献1

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