| 抗HIV蛋白酶抑制剂安普那韦的合成 |
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| 引用本文： | 高玲玲,初秋事,王娟娟,张关永.抗HIV蛋白酶抑制剂安普那韦的合成[J].化学世界,2008,49(2):103-106. |
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| 作者姓名： | 高玲玲 初秋事 王娟娟 张关永 |
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| 作者单位： | 华东理工大学化学与分子工程学院,上海,200237;华东理工大学化学与分子工程学院,上海,200237;华东理工大学化学与分子工程学院,上海,200237;华东理工大学化学与分子工程学院,上海,200237 |
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| 摘 要： | 建立了一条合成抗HIV蛋白酶抑制剂Amprenavir(安普那韦)的路线。以(2S,3R)-N-苄氧羰基-3-氨基-1-氯-4-苯基-2-丁醇为起始原料,经过环氧化、开环取代、胺的酰化、催化氢解还原、胺解等五步反应生成最终产物安普那韦。主要特点在于采用催化氢解还原法,将脱除苄氧羰基保护基和硝基还原成氨基一步完成,使工艺更简单。
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| 关 键 词： | 抗HIV蛋白酶抑制荆 安普那韦 催化氢解 (2S 3R)-N-苄氧羰基-3-氨基-1-氯-4-苯基-2-丁醇 |
| 文章编号： | 0367-6358（2008）02-103-04 |
| 收稿时间： | 2007-04-25 |
| 修稿时间： | 2007-05-24 |
Synthesis and Analysis of HIV Protease Inhibitor Amprenavir |
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| GAO Ling-ling,CHU Qiu-ting,WANG Juan-juan,ZHANG Guan-yong.Synthesis and Analysis of HIV Protease Inhibitor Amprenavir[J].Chemical World,2008,49(2):103-106. |
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| Authors: | GAO Ling-ling CHU Qiu-ting WANG Juan-juan ZHANG Guan-yong |
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| Abstract: | A synthesis method of anti-HIV protease inhibitor Amprenavir was developed.The new route starts from(2S,3R)-N-Cbz-3-amino-1-chloro-4-phenyl-butan-2-ol,and the target compound is obtained through five reactions such as epoxidation reaction,Hinsburg reaction,catalytic hydrogenolysis and ammonolysis reaction.The main point of the research is that the catalytic hydrogenolysis reaction can remove the protected group and reduce the nitro-group to amino-group at the same time to make the reaction more simple. |
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| Keywords: | anti-HIV protease inhibitors Amprenavir catalytic hydrogenolysis (2S 3R)-N-Cbz-3-amino-1-chloro-4-phenyl-butan-2-ol |
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