Highly efficient preparation of aryl β-diketo acids with tert-butyl methyl oxalate
Highly efficient preparation of aryl β-diketo acids with tert-butyl methyl oxalate
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DOI：
10.1021/jo034903x
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发表时间：
2003-09-19
影响因子：
3.6
通讯作者：
Long, YQ
中科院分区：
文献类型：
--
作者：
Jiang, XH;Song, LD;Long, YQ
用草酸甲酯叔丁基完成了芳基甲基酮的改进和高效的草醛化反应。这是构建芳基β -二酮酸药效团的关键一步，芳基β -二酮酸代表了一种有前途的新型HIV-1整合酶抑制剂。结构多样的芳基-二酮酸，包括双二酮酸，可以在温和的条件下以惊人的产量快速制备。草酸二甲酯（或二乙酯）在产率和反应时间上均优于传统方法。
An improved and efficient oxalylation of aryl methyl ketones was accomplished with tert-butyl methyl oxalate. This is the key step in constructing the pharmacophore of aryl beta-diketo acids, which represent a promising new class of HIV-1 integrase inhibitors. Structurally diverse aryl beta-diketo acids, including bisdiketo acids, can be prepared rapidly in impressive yields under mild conditions with this method. Advantages over conventional methods with dimethyl (or diethyl) oxalate were observed in both yield and reaction time.