| 三羰基锝配体基苯基甲磺酰胺的合成与表征 |
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| 引用本文： | 陈永师,林建国,邱玲,程文,罗世能,马海霞.三羰基锝配体基苯基甲磺酰胺的合成与表征[J].应用化学,2012,29(7):757-761. |
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| 作者姓名： | 陈永师 林建国 邱玲 程文 罗世能 马海霞 |
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| 作者单位： | (1.西北大学化工学院 西安 710069；
2.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 无锡 214063) |
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| 基金项目： | 国家自然科学基金，江苏省卫生厅科研项目，2010年度江苏省“企业博士积聚计划”项目 |
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| 摘 要： | 以2-氨基-5-硝基苯酚为原料经过酚羟基烷基化、氨基甲磺酰化、硝基还原为氨基后，进行溴乙酰化以及N-烷基化5步反应制得了三羰基锝标记配体基：N-2-环己基甲氧基-4(1-(2,2′-二吡啶甲基)胺基)乙酰胺基]苯基甲磺酰胺(NSC-PA)，并对反应条件进行了优化。 中间体及目标化合物经红外、质谱和核磁共振氢谱进行了结构表征，HPLC法测定最终产物的纯度大于98%。 该目标化合物可以作为三羰基锝标记前体，为进一步开发乳腺癌显像药物奠定了基础。
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| 关 键 词： | 苯基甲磺酰胺 合成 表征 标记前体 |
| 收稿时间： | 2011-07-25 |
| 修稿时间： | 2011-10-20 |
Synthesis and Characterization of Phenylmethanesulfonamide Ligand for Potential Labeling [99m Tc( CO)3( H2O)3]+ |
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| CHEN Yongshi
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LIN Jianguo
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QIU Ling
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CHENG Wen
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LUO Shineng
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MA Haixia.Synthesis and Characterization of Phenylmethanesulfonamide Ligand for Potential Labeling [99m Tc( CO)3( H2O)3]+[J].Chinese Journal of Applied Chemistry,2012,29(7):757-761. |
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| Authors: | CHEN Yongshi LIN Jianguo QIU Ling CHENG Wen LUO Shineng MA Haixia |
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| Institution: | (1.School of Chemical Engineering,Northwest University,Xi′an 710069,China;
2.Key Laboratory of Nuclear Medicine of Ministry of Healthy,Jiangsu Key Laboratory of ;
Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi 214063) |
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| Abstract: | A new ligand N-2-cyclohexylmethoxy-4(1-(2,2′-bipyridinemethyl)amino)acetylamino] phenylmethanesulfonamide(NSC-PA), for potential labeling 99mTc(CO)3(H2O)3]+ was synthesized by hydroxyl-alkylation, amino-methylsulfonylation, nitro-reduction, amino-bromideacetylation and N- alkylation from 2-amino-5-nitrophenol. Simple experimental operation, short period and purified products could be obtained under optimized conditions. The structures of all the compounds were confirmed by 1H NMR, IR and MS. The purity of the target compound was over 98% as given by HPLC result. The target product could be used for future labeling studies. This synthesis is promising in the exploration of new imaging reagent for breast cancer. |
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| Keywords: | phenylmethanesulfonamide synthesis optimization labeling ligand |
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