| 2-氨基-6-烷氧基嘌呤的合成 |
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| 引用本文： | 陆鸿飞,陆明,吕春绪,章丽娟.2-氨基-6-烷氧基嘌呤的合成[J].精细化工,2006,23(11):1104-1107. |
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| 作者姓名： | 陆鸿飞 陆明 吕春绪 章丽娟 |
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| 作者单位： | 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-烷氧基嘌呤是重要的核苷类药物的中间体。以鸟嘌呤为原料,通过酰化制得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(Ⅱ),收率75.8%。通过2-氨基-6-氯嘌呤(Ⅱ)与醇钠反应得到2-氨基-6-甲氧基嘌呤(Ⅲa),收率96.5%;2-氨基-6-乙氧基嘌呤(Ⅲb),收率79.6%;2-氨基-6-异丙氧基嘌呤(Ⅲc),收率73.2%;2-氨基-6-三氟乙氧基嘌呤(Ⅲd),收率49.8%。用元素分析,核磁共振,质谱,红外光谱对所得产品进行了分析,证明所得产品为目标产品。重点研究了2-氨基-6-三氟乙氧基嘌呤(Ⅲd)的合成,其合成的最佳工艺条件为:n(Ⅱ)∶n(NaOCH2CF3)=1∶5,用二甲亚砜(DMSO)作为反应溶剂,其用量为m(DMSO)∶m(Ⅱ)=13∶1,用碘化亚铜(CuI)为催化剂,其用量为n(CuI)∶n(Ⅱ)=2∶1,反应温度为160℃。
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| 关 键 词： | 嘌呤衍生物 烷氧基化 |
| 文章编号： | 1003-5214（2006）11-1104-04 |
| 收稿时间： | 2006-04-20 |
| 修稿时间： | 2006-04-202006-07-04 |
Synthesis of 2-Amino-6-alkoxypurine |
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| LU Hong-fei,LU Ming,L Chun-xu,ZHANG Li-juan.Synthesis of 2-Amino-6-alkoxypurine[J].Fine Chemicals,2006,23(11):1104-1107. |
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| Authors: | LU Hong-fei LU Ming L Chun-xu ZHANG Li-juan |
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| Affiliation: | LU Hong-fei,LU Ming,L(U) Chun-xu,ZHANG Li-juan |
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| Abstract: | 2-Amino-6-alkoxypurine is an important intermediate of nucleotide.From guanine,through acylation,chloridization and hydrolysis,2-amino-6-chloropurine(Ⅱ,75.8% yield) was obtained Reaction of Ⅱ with a series of so dium alkoxides gave 2-amino-6-methoxypurine(Ⅲa,96.5% yield),2-amino6-ethoxypurine(Ⅲb,79.6% yield),2-amino-6-isopropoxypurine(Ⅲc,73.2% yield) and 2-amino-6-triflouroethoxypurine(Ⅲd,49.8% yield).The products were characterized by elementary analysis,~1HNMR,MS and IR.Ⅲd was studied emphatically,and the best reaction conditions were:n(Ⅱ)∶n(NaOCH_2CF_3)=1∶5,DMSO as solvent,m(DMSO)∶m(Ⅱ)=13∶1,CuI as catalyst,n(CuI)∶n(Ⅱ)=2∶1 and reaction temperature 160 ℃. |
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| Keywords: | purine derivatives alkoxy reaction |
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