| EGF受体配基N2S2-Quinazoline的合成 |
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| 引用本文： | 张建康,周杏琴,钦晓峰,徐希杰,邹美芬.EGF受体配基N2S2-Quinazoline的合成[J].化学试剂,2012,34(9):836-838. |
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| 作者姓名： | 张建康 周杏琴 钦晓峰 徐希杰 邹美芬 |
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| 作者单位： | 江苏省原子医学研究所卫生部核医学重点实验室江苏省分子核医学重点实验室,江苏无锡,214063 |
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| 基金项目： | 卫生部核医学重点实验室青年基金资助项目 |
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| 摘 要： | 以6-硝基喹唑啉酮为原料,经过氯化亚砜氯化,间碘苯胺连接,氯化亚锡还原,制得6-氨基-4-(3-碘苯基)氨基]-喹唑啉,再与氯乙酰氯反应,二硫二氮缩合连接,最后与醋酸汞硫化氢反应脱巯基保护基得到标记前体N-4-(3-碘苯基)氨基]-喹唑啉-6-基]-2-N-(2-巯基乙基)-N-N-(2-巯基乙基)氨基]甲酰甲基]]乙酰胺,主要产物得到核磁和质谱表征,总收率2.5%。
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| 关 键 词： | EGF受体 喹唑啉 双氨基乙硫醇类 合成 |
Synthesis of EGF receptor ligand of N2S2-Quinazoline |
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| ZHANG Jian-kang
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ZHOU Xing-qin
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QIN Xiao-feng
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XU Xi-jie
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ZOU Mei-fen.Synthesis of EGF receptor ligand of N2S2-Quinazoline[J].Chemical Reagents,2012,34(9):836-838. |
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| Authors: | ZHANG Jian-kang ZHOU Xing-qin QIN Xiao-feng XU Xi-jie ZOU Mei-fen |
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| Affiliation: | (Key Laboratory of Nuclear Medicine,Ministry of Health,Jiangsu Key Laboratory of Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi 214063,China) |
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| Abstract: | The labeling precursor of N-4-(3-iodophenyl)amino]-quinazoline-6-yl]-2-N-(2-mercaptoethyl)-N-N-(2-mercaptoethyl)amino]formylmethyl]]acetamide(N2S2-Quinazoline) was synthesized from 6-nitroquinazolone via chlorination with thionyl chloride,condensation with 3-iodoaniline,reduction with stannous chloride dihydrate,reaction with chloroacetyl chloride,joint with N2S2,and then deblocking protecting group with Hg(OAc)2 and H2S.The structures of the compounds were confirmed by 1HNMR and MS.The total yield was about 2.5%. |
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| Keywords: | EGF receptor quinazoline bis(aminoethanethiol) analog synthesis |
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