期刊文献+

盐酸西那卡塞合成新方法 被引量:3

New method for the synthesis of cinacalcet hydrochloride
下载PDF
导出
摘要 目的探讨合成盐酸西那卡塞的新方法。方法以3-(3-三氟甲基苯基)丙醇为原料,经二甲基亚砜/五氧化二磷氧化成醛、三氟甲磺酸铁催化的还原氨化、成盐三步反应,合成了盐酸西那卡塞。结果及结论该方法采用对环境友好的反应试剂,反应步骤少,操作简单,总收率高(57.8%)。 Objective A new method was developed for the synthesis of cinacalcet hydrochloride. Methods Cinacal-cet hydrochloride was prepared from 3 -(3 - trifluoromethylphenyl)- 1 - propanol via three steps,including DMSO/ P2 O5 mediated oxidation,iron triflate catalyzed reductive amination of aldehydes using sodium borohydride,and finally hydrochlo-ride formation. Results and Conclusion This method used environmentally benign reagents to prepare cinacalcet hydro-chloride in only three steps with an overall good yield of 57. 8% .
作者 刘伟 刘兆鹏
机构地区 山东大学药学院
出处 《药学研究》 CAS 2016年第7期425-426,430,共3页 Journal of Pharmaceutical Research
关键词 盐酸西那卡塞 合成 催化还原氨化 Cinacalcet Hydrochloride Synthesis Catalytic reductive amination
  • 相关文献

参考文献13

  • 1NEMETH E F,HEATON W H,MILLER M,et al. Pharmacodynamicsof the type II calcimimetic compound cinacalcetHCl[J] .J Pharmacol Exp Ther,2004,308(2) :27 -635.
  • 2NAGANO N. Pharmacological and clinical properties ofcalcimimetics : calcium receptor activators that afford aninnovative approach to controlling hyperparathyroidism[J]. Pharmacol Ther,2 0 0 6 , 1 0 9 ( 3 ) :339 -365.
  • 3SORBERAL A , CASTANER R M, BAYES M. Cinacalcethydrochloride : Treatment of hyperparathyroidism [J]. DrugFuture,2 0 0 2 , 2 7 ( 9 ) :31 -836.
  • 4胡键,董菁,施小新.盐酸西那卡塞的合成[J].中国医药工业杂志,2010,41(7):488-490. 被引量:12
  • 5李林羚,胡雪峰,杨玉雷,朱雪焱,袁哲东.盐酸西那卡塞的工艺研究[J].中国新药杂志,2013,22(7):834-836. 被引量:17
  • 6卞学国,王均伟,朱启华,徐云根.盐酸西那卡塞的合成工艺研究[J].药物化学,2014,2(1):1-5. 被引量:2
  • 7THIEL 0 R, BERNARD C,TORMOS W ,et al. Practicalsynthesis of the calcimimetic agent, cinacalcet [J]. TetrahedronLett,2008,49(1) :13 -15.
  • 8BIJUKUMAR G , MALOYESH B , BHASKAR B S , et al.Efficient synthesis of cinacalcet hydrochloride [J]. SyntheticCommun,2008,38( 10) :1512 -1517.
  • 9LIFSHITZ - LIRONR,EISENSTADT A ,WIZEL S,et al.Process for preparing of cinacalcet hydrochloride :W0 2 0 0 6 1 2 5 0 2 6 [P].2006 - 1 1 -23.
  • 10ARAVA V R,G0 RENTLA L,DUBEY P K. A novel asymmetricsynthesis of cinacalcet hydrochloride [J]. BeilsteinJ Org Chem,2 0 1 2 ( 8 ) :1366 -1373.

二级参考文献27

  • 1Nemeth EF,Steffey ME,Hammerland LG,et al.Calcimimetics with potent and selective activity on the parathyroid calcium receptor[J].Proc Natl Acad Sci U S A,1998,95(7):4040-4045.
  • 2Nemeth EF,Heaton WH,Miller M,et al.Pharmacodynamics of the type Ⅱ calcimimetic compounds cinacalcet HCI[J].J Pharmacol Exp Ther,2004,308 (2):627-635.
  • 3Nemeth EE Van Wagenen BC,Balandrin MF,et al.Calcium receptor-active molecules:US,6011068[P].2000-01-04.
  • 4Van Wagenen BC,Moe ST,Balandrin ME et al.Calcium receptor-active compounds:US,6211244[P].2001-04-03.
  • 5Thiel OR,Bernard C,Tormos W,et al.Practical synthesis of the calcimimetic agent,cinacalcet[J].Tetrahedron Lett,2008,49(1):13-15.
  • 6Bijukumar G,Maloyesh B,Bhaskar BS,et al.Efficient synthesis of cinacalcet hydrochloride[J].Synth Commun,2008,38(10):1512-1517.
  • 7Lifshitz-liron R,Eisenstadt A,Wizel S,et al.Process for preparing cinacalcet hydrochloride:WO,2006125026[P].2006-11-23.
  • 8NAGANO N. Pharmacological and clinical properties of calcimimetics: Calcium receptor activations that afford an innovative ap- proach to controlling hyperparathyroidism [J]. Pharmacol Ther, 2006, 109(3): 339-365.
  • 9NEMETH EF, HEATON WH, MILLER M, et al. Pharmacodynamics of the type Ⅱ calcimimetic compound cinacalcet HCI[J]. J Pharmacol Exp Ther, 2004, 308 (2) :627 - 635.
  • 10SANDOZ AG. Procee for the preparation of cinacalcet hydrochloride: EP, 1990333 [P]. 2008 - 12 - 11.

共引文献22

同被引文献7

引证文献3

二级引证文献5

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