[1]喻理德,崔汉峰,王星,等.受体酪氨酸激酶抑制剂Dovitinib的合成[J].江西师范大学学报(自然科学版),2013,(02):152-154.
 YU Li-de,CUI Han-feng,WANG Xing,et al.The Synthesis of Tyosine Kinase Inhibitor Dovitinib[J].,2013,(02):152-154.
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受体酪氨酸激酶抑制剂Dovitinib的合成()
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《江西师范大学学报》(自然科学版)[ISSN:1006-6977/CN:61-1281/TN]

卷:
期数:
2013年02期
页码:
152-154
栏目:
出版日期:
2013-03-01

文章信息/Info

Title:
The Synthesis of Tyosine Kinase Inhibitor Dovitinib
作者:
喻理德;崔汉峰;王星;袁金斌
江西中医学院药物中间体合成中心,江西南昌,330004
Author(s):
YU Li-de;CUI Han-feng;WANG Xing;YUAN Jin-bin
关键词:
Dovitinib抗肿瘤药酪氨酸激酶抑制剂合成
Keywords:
dovitinibantitumortyrosine kinase inhibitorsynthesis
分类号:
R914.5
文献标志码:
A
摘要:
5-氟-2-硝基苯胺经N-甲基哌嗪取代,氢气还原,与3-乙氧基-3-亚氨基丙酸乙酯盐酸盐环合,最后与2-氨基-6-氟苯腈反应得Dovitinib,产物收率为43.6;,液相纯度达99.53;.目标产物结构经氢谱、质谱证实.
Abstract:
By substituting 5-chloro-2-nitroaniline by N-methylpiperazine and reduced eby hydrogen,dovitinib is obtained via two cyclizations.The target product structure is confirmed by hydrogen spectrum,mass spectrometry with yield 43%,and liquid purity to 99.53%.

参考文献/References:

[1] 茆勇军,李海泓,李剑峰,等.蛋白酪氨酸激酶信号转导途径与抗肿瘤药物 [J].药学学报,2008,43(4):323-334.
[2] Arora A,Scholar E M.Role of tyrosine kinase inhibitors in cancertherapy [J].J Pharmacol Exp Ther,2005,315(3):971-979.
[3] Sarker D,Molife R,Evans T R J,et al.A phase I pharmaco-kinetic and pharmacodynamic study of TKI258,an ora,l multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors [J].Clin Cancer Res,2008,14(7):2075-2081.
[4] John B Hynes,Alpana Pathak,Constantina H Panes,et al.Direct synthesis of 2,4-diaminoquinazolines from 2-fluorobenzonitriles [J].Journal of Heterocyclic Chemistry,1988,25(4):1173-1177.
[5] Dieter H Klaubert,John H Sellstedt,Charles J Guinosso,et al.N-(Aminopheny1)oxamic acids and esters as potent,orally active antiallergy agents [J].Journal of Medicinal Chemistry,1981,24(6):742-748.
[6] Calvin G,Harwood E,Ryckman D,et al.Methods for synthesizing heterocyclic compounds:WO,2006125130 [P].2006-11-23.
[7] 喻理德,崔汉峰,袁金斌,等.异丁基硼酸的超声辐射合成 [J].江西师范大学学报:自然科学版,2012,36(14):415-416.
[8] William R Antonios-McCrea,Kelly A Frazier,Elisa M Jazan,et al.LHMDS mediated tandem acylation-cyclization of 2-aminobenzenecarbonitriles with 2-benzymidazol-2-yl acetates:a short and efficient route to the synthesis of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones [J].Tetrahedron Letters,2006,47:657-660.
[9] Paul A Renhowe,Sabina Pecchi,Cynthia M Shafer,et al.Design,structure-activity relationships and in vivo characterization 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones:A novel class of receptor tyrosine kinase inhibitors [J].Journal of Medicinal Chemistry,2009,52(2):278-292.

备注/Memo

备注/Memo:
江西省教育厅青年科学基金(GJJ12538)
更新日期/Last Update: 1900-01-01