| N-(4-羟苯基)维甲酰胺的生物素标记衍生物的合成 |
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| 引用本文： | 时彦华,郑友广,吉民. N-(4-羟苯基)维甲酰胺的生物素标记衍生物的合成[J]. 东南大学学报(自然科学版), 2010, 40(2). DOI: 10.3969/j.issn.1001-0505.2010.02.032 |
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| 作者姓名： | 时彦华 郑友广 吉民 |
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| 作者单位： | 东南大学生物科学与医学工程学院,南京,210009;东南大学苏州研究院苏州市生物医用材料与技术重点实验室,苏州,215123;东南大学苏州研究院苏州市生物医用材料与技术重点实验室,苏州,215123;东南大学化学化工学院,南京,210009;东南大学生物科学与医学工程学院,南京,210009;东南大学苏州研究院苏州市生物医用材料与技术重点实验室,苏州,215123;东南大学化学化工学院,南京,210009 |
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| 摘 要： | 为了研究抗肿瘤药物N-(4-羟苯基)维甲酰胺(4-HPR)的作用机理和其生物学作用靶点,合成了4-HPR的生物素衍生物.采用全反式维甲酸与草酰氯反应生成酰氯,再与三乙胺成盐,然后将得到的酰基铵盐,与对氨基苯酚发生酰胺化反应,制得4-HPR.4-HPR与3-溴-1-丙醇烷基化反应得到含羟基链化合物,4-氨基丁酸与生物素发生酰胺化反应得到羧酸化合物.最后通过酯化反应将4-HPR与生物素连接得到目标化合物.该方法具有操作简单、反应条件温和以及产率较高等特点.
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| 关 键 词： | 4-HPR 生物素标记物 合成 |
Synthesis of biotinylated 4-HPR derivative |
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| Shi Yanhua, Zheng Youguang, Ji Min,. Synthesis of biotinylated 4-HPR derivative[J]. Journal of Southeast University(Natural Science Edition), 2010, 40(2). DOI: 10.3969/j.issn.1001-0505.2010.02.032 |
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| Authors: | Shi Yanhua Zheng Youguang Ji Min |
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| Affiliation: | 1School of Biological Science and Medical Engineering;Southeast University;Nanjing 210009;China;2Suzhou Key Laboratory of Biomedical Materials and Technology of Research Institute;Suzhou 215123;China;3School of Chemistry and Chemical Engineering;China |
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| Abstract: | A biotinylated derivative of N-(4-hydroxyphenyl) retinamide(4-HPR) was synthesized to further understand its biological mechanisms and to identify its target proteins.It consists of the preferred steps of reacting all-trans retinoic acid with oxalyl chloride to form retinoyl chloride and then reacting with triethylamine to generate retinoyl ammonium salt which in turn is reacted with paminophenol to eventually produce 4-HPR.4-HPR is treated with 3-bromo-1-propanal to generate the chain product,which then re... |
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| Keywords: | 4-HPR N-(4-hydroxyphenyl) retinamide biotin synthesis |
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