Conversion of 伪-Amino Acids into Bioactive o-Aminoalkyl Resorcylates and Related Dihydroxyisoindolinones
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- 作者：Bhavesh H. Patel ; Andrew M. Mason ; Hetal Patel ; R. Charles Coombes ; Simak Ali ; Anthony G. M. Barrett
- 刊名：Journal of Organic Chemistry
- 出版年：2011
- 出版时间：August 5, 2011
- 年：2011
- 卷：76
- 期：15
- 页码：6209-6217
- 全文大小：939K
- 年卷期：v.76,no.15(August 5, 2011)
- ISSN：1520-6904
文摘
The synthesis of biologically active o-aminoalkyl resorcylates and related dihydroxyisoindolinones from functionalized 伪-amino acids without the use of phenolic protection is described. The key aminoalkyl-diketo-dioxinone intermediates were prepared utilizing a crossed Claisen condensation reaction in the presence of diethylzinc. The aromatic unit was constructed via late stage cyclization and aromatization, and subsequent modification provided the novel resorcylates which showed activity against a selection of receptors and kinases, including 5-HT and CDK.