| An Improved Synthetic Method of Saquinavir |
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| 作者姓名： | YANG Qin-gang HE Xu-chang LEI Li-jun ZHOU Qi-ting BAI Dong-lu |
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| 作者单位： | YANG Qin-gang，HE Xu-chang，LEI Li-jun，ZHOU Qi-ting and BAI Dong-lu ** Shanghai Institute of Materia Medica，Shanghai Institutes of Biological Sciences，Chinese Academy of Sciences，Shanghai 201203，P. R. China |
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| 基金项目： | Supported by the Science and Technology Commission of Shanghai Municipality（ No. 024319126）. |
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| 摘 要： | IntroductionThe human immunodeficiency virus(HIV)is thecausative agent of acquired immunodeficiency syndrome(AIDS).Since HIV protease is essential for the repli-cation and maturation of HIV,the inactivation of HIVprotease by either mutation or chemical in…
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| 关 键 词： | 合成方法 蛋白酶抑制剂 HIV 沙奎那韦 |
| 文章编号： | 1005-9040（2006）-01-051-05 |
| 收稿时间： | 2005-03-01 |
An Improved Synthetic Method of Saquinavir |
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| YANG Qin-gang HE Xu-chang LEI Li-jun ZHOU Qi-ting BAI Dong-lu.An Improved Synthetic Method of Saquinavir[J].Chemical Research in Chinese University,2006,22(1):51-55. |
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| Authors: | Qin-gang YANG Xu-chang HE Li-jun LEI Qi-ting ZHOU Dong-lu BAI |
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| Institution: | Shanghai Institute of Materia Medica, Shanghai Institutes of Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, P. R. China |
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| Abstract: | An improved synthetic method of saquinavir, an HIV protease inhibitor, is described. In comparison with the methods in the reported works, the improved procedures had several advantages, such as less expensive agents, shorter reaction time, and a smaller amount of the solvent needed. To measure the optical purities of the products, the intermediates were determined by means of chiral HPLC. Some of the intermediates can also be used for the preparation of new protease inhibitors. |
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| Keywords: | HIV Protease inhibitor Saquinavir Synthesis |
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