A simple and highly efficient preparation of structurally diverse Aryl beta-diketoacids as HIV-1 integrase inhibitors
文献类型：期刊论文
| 作者 | Jiang, XH; Long, YQ |
| 刊名 | CHINESE JOURNAL OF CHEMISTRY
 |
| 出版日期 | 2004-09 |
| 卷号 | 22期号:9页码:978-983 |
| 关键词 | oxalylation sodium tert-butoxide dimethyl oxalate aryl beta-diketoacid HIV-1 integrase inhibitor bis-diketoacid |
| ISSN号 | 1001-604X |
| 文献子类 | Article |
| 英文摘要 | In order to provide a facile and practical access to structurally diverse aryl beta-diketoacids, An improved and highly efficient oxalylation method was developed which employed commercially available and cheap reagents. The oxalylation of aryl methyl ketones, the key step to construct the pharmacophore of aryl beta-diketoacids, was considerably facilitated by a new combination of dimethyl oxalate as an oxalic source and sodium tert-butoxide as a base. A wide variety of aryl beta-diketoacids bearing different functional groups can be prepared rapidly in high yields at room temperature with this method, which has significant advantages over the previously reported procedures in a wider application range, much less amount of reagents, pretty higher yields and quite shorter reaction time. The bis-aryldiketoacids 3k and 3l, readily prepared by this method, displayed interesting and promising inhibitory activities against HIV-1 integrase and HIV-1 replication in cells. |
| WOS关键词 | REPLICATION ; DERIVATIVES ; DESIGN ; ACIDS ; CELLS |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000223842000020 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274023]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Long, YQ |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, XH,Long, YQ. A simple and highly efficient preparation of structurally diverse Aryl beta-diketoacids as HIV-1 integrase inhibitors[J]. CHINESE JOURNAL OF CHEMISTRY,2004,22(9):978-983. |
| APA | Jiang, XH,&Long, YQ.(2004).A simple and highly efficient preparation of structurally diverse Aryl beta-diketoacids as HIV-1 integrase inhibitors.CHINESE JOURNAL OF CHEMISTRY,22(9),978-983. |
| MLA | Jiang, XH,et al."A simple and highly efficient preparation of structurally diverse Aryl beta-diketoacids as HIV-1 integrase inhibitors".CHINESE JOURNAL OF CHEMISTRY 22.9(2004):978-983. |
入库方式： OAI收割
来源：上海药物研究所
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