| A Convenient Synthesis of cis and trans-(±)-4-Amino-1-[2-(hydroxyl-methyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone |
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| 作者姓名： | Yi SHEN Ling XIANG Yong DENG Yu Guo ZHONG |
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| 作者单位： | Yi SHEN，Ling XIANG，Yong DENG，Yu Guo ZHONG Department of Medicinal Chemistry，West China School of Pharmacy，Sichuan University，Chengdu 610041 |
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| 摘 要： | A convenient synthesis of cis-(±) isomer 1 and trans-(±) isomer 2 of lamivudine starting from benzoyloxyacetaldehyde and l,4-dithiane-2,5-diol is described. The key steps include chlorination of oxathiolane lactol 5 by SOCl2/DMF, followed by coupling with silylated N4-acetylcytosine and deprotection. The overall yield was 42.6 % and 20.1 %, respectively.
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| 关 键 词： | Lamivudine geometrical isomer cis-(±) isomer trans-(±) isomer synthesis. |
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