| N-[3',3'-双(膦羧基)丙基]-3-{4-[双(2-氯乙基)氨基]苯基}-3-氨基丙酰胺的合成及表征 |
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| 引用本文： | 安丽莉,曾建成,吴勇.N-[3',3'-双(膦羧基)丙基]-3-{4-[双(2-氯乙基)氨基]苯基}-3-氨基丙酰胺的合成及表征[J].华西药学杂志,2006,21(2):118-120. |
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| 作者姓名： | 安丽莉 曾建成 吴勇 |
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| 作者单位： | 四川大学华西药学院,四川 成都 610041 |
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| 摘 要： | 目的合成N-3’,3’-双(膦羧基)丙基]-3-{4-双(2-氯乙基)氨基]苯基}-3-氨基丙酰胺,并进行体外骨靶向性实验。方法以3,3-双(二乙氧膦酰基)-1-硝基丙烷(1)为原料,经氢化还原,再与N-苄氧羰酰异苯丙氨酸氮芥(2)偶联,催化氢化还原得到化合物(4),用溴代三甲基硅烷脱去膦酸酯的烷基得到目标化合物T。用羟磷灰石晶体作为骨模型,测定偶联物T的趋骨性。结果和结论目标物T经1HNMRI、R、MS得到结构确证,体外骨靶向性实验显示,目标物T有良好的骨靶向性。
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| 关 键 词： | 3 3-双(二乙氧膦酰基)丙基胺 N-苄氧羰酰异苯丙氨酸氮芥 合成 骨靶向 趋骨性 |
| 文章编号： | 1006-0103(2006)02-0118-03 |
| 收稿时间： | 2005-07 |
| 修稿时间： | 2005年7月1日 |
Synthesis and bone-targeted study of N-[3',3'-di(phosphonoxy)propyl]-3-{4-[bis(2-chloroethyl)Amino]phenyl}-3-aminopropionamide |
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| AN Li-li,ZENG Jian-cheng,WU Yong.Synthesis and bone-targeted study of N-[3'''',3''''-di(phosphonoxy)propyl]-3-{4-[bis(2-chloroethyl)Amino]phenyl}-3-aminopropionamide[J].West China Journal of Pharmaceutical Sciences,2006,21(2):118-120. |
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| Authors: | AN Li-li ZENG Jian-cheng WU Yong |
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| Institution: | 1. West China School of Pharmacy, Sichuan University, Chengdu 610041, China;2.West China Hospital of Sichuan University, Chengdu 610041, China |
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| Abstract: | OBJECTIVE To synthesize N-3',3'-di(phosphonoxy)propyl]3-{4-bis(2-chloroethyl)amino]phenyl}-3-aminopropionamide and test its bone targeting characters in vitro.METHODS 3,3-di(phosphonoxy)propyl-amino(1) with hydrogenation was conjugated with N-benzyloxcarbonyl Betamerphalan(2),followed by catalytic hydrogenation for intermediate(4).Then the title conjugate T was obtained via dealkylation of phospho rate(4) by using trimethysilyl bromide.RESULTS and CONCLUSION The structure of title conjugate T was verified by()~1HNMR,IR and MS.It showed good bone-seeking ability via hydroxyapatite adhesion tests in vitro. |
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| Keywords: | 3 3-di(phosphonoxy)propylamino N-benzyloxcarbonyl betamerphalan Synthesis Bone-targeted Dealkylation |
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