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钯催化偶合卟吩-并合杂环顺烯二炔二联体的合成
引用本文:殷军港,王进军,沈荣基. 钯催化偶合卟吩-并合杂环顺烯二炔二联体的合成[J]. 高等学校化学学报, 2005, 26(8): 1474-1476
作者姓名:殷军港  王进军  沈荣基
作者单位:1. 兰州大学化学化工学院, 兰州730000;2. 烟台大学应用化学系, 烟台265005;3. 韩国仁济大学, 釜山
基金项目:中-韩合作项目;山东省技术创新项目
摘    要:具有新颖共轭顺-烯二炔结构的天然产物可精巧地引发顺-烯二炔的闭环反应而产生双自由基,从癌细胞DNA糖磷脂骨架上夺取氢原子,促成病变细胞氧化断裂而产生强烈的抗癌功效(比阿霉素抗癌活性大4000倍)。作为保证抗肿瘤疗效的另一重要因素是提高抗癌药物对病变组织的选择性,基于用于光动力疗法(PDT)的抗癌药物卟啉类化合物识别和选择性富集于肿瘤细胞的特殊功能,

关 键 词:偶联反应  焦脱镁叶绿酸  卟吩-顺烯二炔二联体  光动力疗法  
文章编号:0251-0790(2005)08-1474-03
收稿时间:2004-08-26
修稿时间:2004-08-26

Synthesis of Chlorin-enediyne Dyads Fused with Heterocyclic Ring by Palladium-catalyzed Coupling Reaction
YIN Jun-Gang,WANG Jin-Jun,SHIM Young-Key. Synthesis of Chlorin-enediyne Dyads Fused with Heterocyclic Ring by Palladium-catalyzed Coupling Reaction[J]. Chemical Research In Chinese Universities, 2005, 26(8): 1474-1476
Authors:YIN Jun-Gang  WANG Jin-Jun  SHIM Young-Key
Affiliation:1. Collgeg of Chemistry and Chemical Engineering, Lanzhou 730000, China;2. Department of Applied Chemistry, Yantai University, Yantai 264005, China;3. School of Nano Engineering, Inji University, Pusan, Korea
Abstract:The terminal alkyne was constructed in chlorin chromophore by Grignard reaction and oxidation to give chlorin 2 and 3, respectively. After deprotection the diketo chlorin 4 was obtained which was readily converted to the Zn-complex 5. Chlorin-enediyne dyads 6 fused with heterocyclic ring was synthesized by a palladium-catalyzed coupling reaction with 2-(1-hexynyl)-3-chlorothiophene.
Keywords:Coupling reaction   Pyropheophorbide   Chlorin-enediyne dyads   Photodynamic therapy
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