期刊文献+

异环磷酰胺的合成 被引量:2

Synthesis of Ifosfamide
下载PDF
导出
摘要 3-氨基丙醇与三氯氧磷环合制得2-氯四氢-2H-1,3,2-氧氮磷杂环己烯-2-氧化物,然后与2-氯乙胺盐酸盐进行烷基化反应,继而经氯乙酰氯酰化得3-(2-氯乙酰基)-2-[(2-氯乙基)氨基]四氢-2H-1,3,2-氧氮磷杂环己烯-2-氧化物,最后经硼氢化钠/浓硫酸还原得到抗肿瘤药异环磷酰胺,总收率为30%(以3-氨基丙醇计)。 Ifosfamide was synthesized from 3-aminopropanol by cyclization to give 2-chlorotetrahydro-2H- 1,3,2-oxazaphosphorine-2-oxide, which was alkylated with 2-chloroethylamine hydrochloride, acylated with chloroacetyl chloride, and then reduced by NaBH4/H2SO4 in 30 % overall yield.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2009年第7期483-485,共3页 Chinese Journal of Pharmaceuticals
关键词 异环磷酰胺 抗肿瘤药 合成 ifosfamide antitumor agent synthesis
  • 相关文献

参考文献9

  • 1彭浩.异环磷酰胺[J].中国新药杂志,1997,6(1):37-37. 被引量:6
  • 2衣淑珍.异环磷酰胺临床研究进展[A].2006第六届中国药学会学术年会论文集[C].广州:中国药学会,2006:494-496.
  • 3Van Masnen JMS,Griggs L J,Jarman M.Synthesis of 14C-labelled isophosphamide[J].J Label Compd Radiopharm,1981,18 (3):385-390.
  • 4汤磊,周训蓉,王建塔,李秀广.异环磷酰胺的合成[J].中国医药工业杂志,2006,37(8):513-514. 被引量:2
  • 5Arnold H,Brock N,Bourseaus F,et al,N',O-Propylene phosphoric acid ester diamides:US,3732340[P].1973-05-08.
  • 6尼米耶尔U,尼格尔H,库彻尔B,等.制备氧氮杂膦-2-胺的方法:中国,1268950[P].2000-10-04.
  • 7Iwamoto RH,Acton EM,Goodman L,et al.Potential anticancer agents.LXIV.Alkylating agents related to phenylalanine mustard.V.A cyclic phosphorodiamidate related to cytoxan[J].J Org Chem,1961,26(11):4743-4745.
  • 8Pankiewiez K,Kinas R,Stec W J,et al.Synthesis and absolute configuration assignments of enantiomeric forms of ifosphamide,sulfosphamide,and trofosphamide[J].J Am Chem Soc,1979,101 (26):7712-7718.
  • 9Dyer UC,Brennan JJ.The preparation of Ifosfamide and analogues:WO,9624600[P].1996-08-15.

二级参考文献6

  • 1Van Masnen JMS,Griggs LJ,Jarman M.Synthesis of ^14Clabelled isophosphamide[J].J Labelled Compd Radiopharm,1981,18(3):385-390.
  • 2Arnold H,Brock N,Bourseaus F,et al.N',O-Propylene phosphoric acid ester diamides[P].US:3732340,1973-05-08.
  • 3尼米耶尔U 尼格尔H 库彻尔B 等.制备氧氮杂膦—2—胺的方法[P].CN:98808752,1998—08—14[J].CA,1999,130:1252-1252.
  • 4Philip AL,William AP,Melvin LR.A modification of Wenker's method of preparing ethyleneimine[J].J Am Chem Soc,1947,69(6):1540-1540.
  • 5Wystrach VP,Donald WK,Fred CS.Preparation of ethylenimine and triethylenemelamine[J].J Am Chem Soc,1955,77(22):5915-5918.
  • 6Pankiewicz K,Kinas R,Stec WJ,et al.Synthesis and absolute configuration assignments of enantiomeric forms of ifosphamide,sulfosphamide,and trofosphamide[J].J Am Chem Soc,1979,101 (26):7712-7718.

共引文献6

同被引文献33

  • 1陈莉莉,岑均达.克拉屈滨的合成[J].中国医药工业杂志,2005,36(7):387-389. 被引量:6
  • 2唐锋,郑国海,姚其正,吕刚,周卫芬,王秋娟.新型甲氨蝶呤衍生物的合成[J].化学学报,2006,64(3):249-254. 被引量:2
  • 3汤磊,周训蓉,王建塔,李秀广.异环磷酰胺的合成[J].中国医药工业杂志,2006,37(8):513-514. 被引量:2
  • 4J.A. Beisler. Isolation, characterization, and properties of a labile hy- drolysis product of the antitumor nucleoside, 5 - azacytidine [ J ]. J. Med. Chem. , 1978,21(2) :204 -208.
  • 5Frantisek Soml, Alois Plskala. Process for the manufacture of 1 - glyco- syl - 5 - azacytosines[ P ]. US:3350388,1963 - 12 -22.
  • 6Piskala, F. Sorm. Synthesis of 5 -azacytidine according to an original paper of Collection[J]. Czech. Chem. Commun, , 1964,29:2 060 -2 076.
  • 7Piskala, F. Sorm. Process of isolating vinblastine from the plant catharabthis mseus[ P], US:4749787,1986 - 10 -23.
  • 8Ioncscu D. , Blumbergs P. Synthesis of 5 - azacytidine via ribosylation of azacytosine[ P]. US :2004186283,2004.
  • 9Ikehara M, Tada H. Studies of nucleosides and nucleotides. XXIV. Pufine cyclonucleosides. I. 8,2' - cyclonucleoside derived from 2 - chloro - 8 - mercapto - 9 - b - D - xylofuranosyladenine[ J]. J. Am. Chem. Soc. , 1965,87(3) :606 -610.
  • 10Christensen LF, Broom AD. Synthesis and biological activity of selected 2,6 - disubstituted - (2 - deoxy - a - and - b - D - erythmpento- furanosyl)purines[J]. J. Med. Chem., 1972,15(7):735-739.

引证文献2

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