A Simple and Highly Efficient Preparation of Structurally Diverse Aryl β-diketoacids as HIV-1 Integrase Inhibitors

• 来源期刊: 中国化学（英文版）
• 年，卷（期）: 2004,（9）
• 页码范围: 978-983
• 页数: 6页
• 语种: 英文

摘要

In order to provide a facile and practical access to structurally diverse aryl β-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 β-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 β-diketoacids bearing different functional groups can be prepared rapidly in high yields at room t. emperature 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 31, readily prepared by this method, displayed interesting and promising inhibitory activities against HIV-1 integrase and HIV-1 replication in cells.