期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

盐酸乙氟利嗪的合成 被引量：1

Synthesis of Efletirizine Hydrochloride
原文传递
导出
摘要 1-[双(4-氟苯基)甲基]哌嗪和氯乙氧基乙酸乙酯在碘化钾催化下,以三乙胺作缚酸剂,于二甲苯中缩合制得2-[2-[4-[双(4-氟苯基)甲基]-1-哌嗪基]乙氧基]乙酸乙酯,再经水解、成盐酸盐制得组胺H1受体拮抗剂盐酸乙氟利嗪,总收率约78%。 Efletirizine hydrochloride,a histamine H1 receptor antagonist,was synthesized from ethyl(2-chloroethoxy)acetate by condensation with 1-[bis(4-fluorophenyl)methyl]piperazine in the presence of potassium iodide and triethylamine in xylene to give ethyl 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetate,followed by hydrolysis and salt formation with an overall yield of about 78%.
作者 杜翔宇 王晰婷 孙海龙 马丽芳
机构地区 四川大学化学工程学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2011年第5期321-323,共3页 Chinese Journal of Pharmaceuticals
关键词 盐酸乙氟利嗪 组胺H1受体拮抗剂 合成 efletirizine hydrochloride histamine H1 receptor antagonist
分类号 R9 [医药卫生—药学]
  • 相关文献

参考文献7

  • 1谭转云,向红琳,杨晓红,周海燕.盐酸西替利嗪的合成工艺改进[J].中南药学,2006,4(5):362-364. 被引量：4
  • 2王新平,李翠翠.盐酸西替利嗪的合成[J].齐鲁药事,2006,25(5):300-302. 被引量：5
  • 3何永志,刘东志.盐酸西替利嗪的合成工艺改进[J].天津医科大学学报,2003,9(4):488-490. 被引量：7
  • 4Berwaer M,Bodson G,Deleers M,et al.Pseudopolymorphicforms of 2-[2-[4-[bis (4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride. WO,9928310 . 1999
  • 5Diouf O,Surtees J.Process for the preparation of2-[2-[4-[bis (4-fluorophenyl)methyl]piperazin-1-yl]-ethoxy]acetic acid derivatives or corresponding salt formsthereof and intermediates therefor. WO,2003009849 . 2003
  • 6Baltes E,Lannoy JD,Rodriguez L.2- (4- (Diphenylmethyl)-1-piperazinyl)-acetic acids and their amides,process for theirpreparation and pharmaceutical compositions. EP,0058146 . 1982
  • 7Ori Lerman,Erez Gal,Joseph Kaspi.Aprocess for the prepara-tion of esters of[2-[4-[(4-chlorophenyl)phenyl methyl]-1-piperazinyl]-ethoxy]acetic acid. EP 0 952 153 . 1999

二级参考文献11

  • 1[1]Baltes E, De Lannoy J, Rodriguez L. 2- [4- (diphenylmethyl) - 1- piperazinyl] acetic acids and their amides and pharmaceutical compositions[p] .Eur Pat Appl: EP58146, 1982 - 08 - 18
  • 2[2]Cossement E, Motte G, Bodson G, et al. Process for prepara tion of cetirizine, its dihydrochloride and optical isomers via hydrolysis and corresponding nitrles[p] .Brit UK Pat Appl: GB2225321, 1900 - 08- 30
  • 3[3]Cossement E, Gobert J, Bodson G Process for preparation of cetirizine and its dihydrochloride via etherification with haloacetates[p]. Brit UK Pat Appl: GB2225320, 1990 - 05 - 30
  • 4[1]Baltes E,De Lannoy J.Rodriguez L.2-[4-(diphenylmethy)-1-piperazinyl]acctic acids and their amides and pharmaceutical compositions[P].EP:58146,1982-08-18.
  • 5[2]Cossement E,Motte G,Bodson G,et al.Process for the preparation of cetirizine,its dihydrochloride and optical isomers via hydrolysis and corresponding nitriles[P].GB:2225321,1990-08-30.
  • 6[3]Cossement E,Motte G,Bodson G,et al.Process for the preparation of cetirizine and its dihydrochloride via etherification with haloacetates[P].GB:2225320,1990-05-30.
  • 7[4]Guy Duchene,Michel Deleers,Guy Bodson,et al.Substituted[2-(1-piperazinyl)-ethoxy] methyl compounds[P].USP 6140501:2000-10-30.
  • 8[7]Ori Lerman,Erez Gal,Joseph Kaspi.A process for the preparation of esters of -[7-[4-[(4-chlorophenyl)phenylmethy]-1-piperazinyl]-ethoxy] acetic acid[P].EP:0952153,1999-10-27.
  • 9陈志刚,徐建华.钾通道开放剂对抗原诱发大鼠肥大细胞释放组胺的抑制作用[J].浙江医科大学学报,1997,26(2):49-51. 被引量：2
  • 10王健君,杨雪艳,吴范宏.盐酸西替利嗪的改进合成[J].华东理工大学学报（自然科学版）,2002,28(6):668-670. 被引量：9

共引文献11

同被引文献33

  • 1朱国东,陆涛.二苯基哌嗪(啶)类化合物的药理作用及研究进展[J].药学进展,2004,28(9):395-400. 被引量：1
  • 2刘莹,郑腾飞,金凤,周璐,刘振明,魏平,来鲁华.非肽类SARS冠状病毒3CL蛋白酶抑制剂的设计与活性表征[J].化学学报,2007,65(16):1707-1712. 被引量：3
  • 3Reiter J,Trinka P,Bartha FL,et al. New Manufacturing Pro- cedure of Cetirizine [J]. Organic Process Research & De- velopment, 2012, 16 (7) : 1279-1282.
  • 4Nutalapati,Siva RK. Methods of administering combinations of antihistamines for treatment of allergic reactions: US, 20130053399[P].2013-02-28.
  • 5Venkat NA,Narsimha P. Efficient synthesis of antihistamines clocinizine and chlorcyclizine [J]. Medicinal Chemistry Research, 2012,21 (4) : 538-541.
  • 6Brennan AB,Long CJ,Bagan JW,et al. Surface topogra- phies for non-toxic bioadhesion control: US, 2010022 6943[P].2010-09-09.
  • 7Yeap YY, Trevaskis NL, Quach T, et al. Intestinal Bile Secretion Promotes Drug Absorption from Lipid Colloidal Phases via Induction of Supersaturation [J]. Molecular Pharmaeeuties, 2013,10(5) : 1874-1889.
  • 8Moriuchi K.,Takeda Y. Binder composition for electrodes and electrode mix slurry: WO, 2010100945 [P].2010--09--10.
  • 9Ott C, Schneider MP,Raff U, et al. Effects of manidipine vs. amlodipine on intrarenal haemodynamics in patients with arterial hypertension [J]. British Journal of Clinical Pharmacolog, 2013, 75( 1 ) : 129-135.
  • 10Sumizawa T, Chen ZS, Chuman Y, et alo Reversal of mul- tidrug resistance-associated protein-mediated drug re- sistance by the pyridine analog PAK-104P [J]. Molecular pharmacology, 1997,51 (3) : 399-405.

引证文献1

中国医药工业杂志
2011年 第5期

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