| 9-[(4氟-)-3羟-基甲基丁基]鸟嘌呤(FHBG)的改进合成方法 |
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| 引用本文： | 蔡汉成,尹端沚,张岚,汪勇先.9-[(4氟-)-3羟-基甲基丁基]鸟嘌呤(FHBG)的改进合成方法[J].精细化工,2006,23(8):813-816. |
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| 作者姓名： | 蔡汉成 尹端沚 张岚 汪勇先 |
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| 作者单位： | 1. 中国科学院,上海应用物理研究所,放射性药物研究中心,上海,201800;中国科学院,研究生院,北京,100049
2. 中国科学院,上海应用物理研究所,放射性药物研究中心,上海,201800 |
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| 基金项目： | 上海市自然科学基金;中国科学院知识创新工程项目;国家自然科学基金 |
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| 摘 要： | 报道了9-(4氟-)-3羟-基甲基丁基]鸟嘌呤(FHBG,Ⅱ)的改进合成方法,对起始原料喷昔洛韦(Ⅲ)的氨基和一个羟基用4-甲氧基氯化三苯甲烷保护,对另一个羟基磺酯化,得到N2-(p-甲氧基苯酰基二苯基甲基)-9-(4甲-苯磺酰)-3-p-甲氧基苯酰基二苯基-甲氧基甲基丁基]鸟嘌呤(Ⅴ),收率为70.5%;再用四丁基氟化铵(TBAF)对化合物Ⅴ亲核取代4-甲苯磺酰基团,水解脱去保护基,即得FHBG。产品经1HNMR、IR、MS表征,并用HPLC分析了Ⅴ和Ⅱ,保留时间分别为5.89 m in和4.41 m in,积分计算质量分数分别为w(Ⅴ)=99.5%和w(Ⅱ)=99.3%。
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| 关 键 词： | 9-[(4氟-)-3羟-基甲基丁基]鸟嘌呤 正电子发射型计算机断层扫描 报告基因 |
| 文章编号： | 1003-5214（2006）08-0813-04 |
| 收稿时间： | 2006-01-11 |
| 修稿时间： | 2006-01-112006-03-16 |
The Improved Synthesis of 9-[(4-Fluoro)-3-hydroxymethylbutyl] Guanine (FHBG) |
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| CAI Han-cheng,YIN Duan-zhi,ZHANG Lan,WANG Yong-xian.The Improved Synthesis of 9-[(4-Fluoro)-3-hydroxymethylbutyl] Guanine (FHBG)[J].Fine Chemicals,2006,23(8):813-816. |
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| Authors: | CAI Han-cheng YIN Duan-zhi ZHANG Lan WANG Yong-xian |
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| Affiliation: | 1. Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China ;2. Graduate School of the Chinese Academy of Sciences,Beijing 100049, China |
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| Abstract: | The improved synthesis of 9-(4-fluoro)-3-hydroxymethylbutyl] guanine(FHBG,Ⅱ) is reported.Penciclovir(Ⅲ) was converted to ditrityl-penciclovir(Ⅳ) by treatment with methoxytrityl chloride.Ⅳ was transformed to ditrityl-4-tosyl-penciclovir(Ⅴ) by tosylation with high yield(up to 70.5%).Ⅴ reacted with tetrabutylammonium fluoride to afford ditrityl-4-fluoro-penciclovir(Ⅵ).Removal of the methoxytrityl groups in Ⅵ by acidic hydrolysis produced Ⅱ.Structures of the products were characterized by IR,~1HNMR spectra and MS.For the quality control,Ⅱ and Ⅴ were analyzed by HPLC on a reverse-phase C_18 column,eluting at 5.89 min and 4.41 min respectively,to give w(Ⅱ)=99.5% and w(Ⅴ)=99.3% by HPLC area normalization method. |
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| Keywords: | 9-[(4-fluoro)-3-hydroxymethylbutyl] guanine positron emission tomography reporter gene |
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