| 2-氨基-6-卤代嘌呤的合成 |
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| 引用本文： | 陆鸿飞,陆明,吕春绪,贺鹰,张康康.2-氨基-6-卤代嘌呤的合成[J].精细化工,2006,23(4):386-388,392. |
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| 作者姓名： | 陆鸿飞 陆明 吕春绪 贺鹰 张康康 |
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| 作者单位： | 南京理工大学,化工学院,江苏,南京,210094;南京理工大学,化工学院,江苏,南京,210094;南京理工大学,化工学院,江苏,南京,210094;南京理工大学,化工学院,江苏,南京,210094;南京理工大学,化工学院,江苏,南京,210094 |
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| 摘 要： | 2-氨基-6-卤代嘌呤是重要的核苷类药物的中间体。以鸟嘌呤为原料,通过乙酰化制得N2.9-二乙酰鸟嘌呤(Ⅰ),收率95.8%。氯化水解得到2-氨基-6-氯嘌呤(Ⅱa),收率75.8%。通过卤素交换制得2-氨基-6-氟嘌呤(Ⅱb)、2-氨基-6-溴嘌呤(Ⅱc)和2-氨基-6-碘嘌呤(Ⅱd),其收率分别为39.5%,87.2%和91.5%。用元素分析,核磁共振光谱,质谱,红外光谱对产物进行了分析,证明所得产物为目标化合物。重点研究了2-氨基-6-氟嘌呤(Ⅱb)的合成,最佳工艺条件为:n(Ⅱa)∶n(KF)=1∶5,硝基苯为溶剂,m(硝基苯)∶m(Ⅱa)=21∶1,四苯基溴化膦为相转移催化剂,m(四苯基溴化膦)∶m(Ⅱa)=1∶17,反应温度为190℃。
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| 关 键 词： | 嘌呤衍生物 鸟嘌呤 卤素交换 |
| 文章编号： | 1003-5214（2006）04-0386-04 |
| 收稿时间： | 2005-10-14 |
| 修稿时间： | 2005-10-142005-11-18 |
Synthesis of 2-Amino-6-halogenpurine |
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| LU Hong-fei,LU Ming,L Chun-xu,HE Ying,ZHANG Kang-kang.Synthesis of 2-Amino-6-halogenpurine[J].Fine Chemicals,2006,23(4):386-388,392. |
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| Authors: | LU Hong-fei LU Ming L Chun-xu HE Ying ZHANG Kang-kang |
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| Affiliation: | LU Hong-fei,LU Ming,L(U) Chun-xu,HE Ying,ZHANG Kang-kang |
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| Abstract: | 2-Amino-6-halogenpurine is a kind of important semi-pharmic of nucleotide.From guanine,through acetylation,chlorination and hydrolyzation,2-amino-6-chloropurine(Ⅱ_a,yield 75.8%) was produced.Through halogen exchange,2-amino-6-fluoropurine(Ⅱ_b,yield 39.5%),2-amino-6-bromo-purine(Ⅱ_c,yield 87.2%) and 2-amino-6-iodopurine(Ⅱ_d yield,91.5%) are formed.The products were characterized by elementary analysis,~1HNMR,MS and IR.Synthesis of Ⅱ_b was studied emphatically.The best technological conditions were:n(Ⅱ_a)∶n(KF)=1∶5,m(nitrobenzene)∶m(Ⅱ_a)=21∶1,m(Ph_4PBr)∶m(Ⅱ_a)=1∶17 and reaction temperature 190 ℃. |
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| Keywords: | purine derivatives guanine halogen exchange |
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