Regio- and Diastereoselective Construction of 伪-Hydroxy-未-amino Ester Derivatives via 1,4-Conjugate Addition of 尾,纬-Unsaturated N-Sulfonylimines

详细信息    查看全文

• 作者：Lin Qiu ; Lixin Gao ; Jixing Tang ; Dongwei Wang ; Xin Guo ; Shunying Liu ; Liping Yang ; Jia Li ; Wenhao Hu
• 刊名：Journal of Organic Chemistry
• 出版年：2014
• 出版时间：May 2, 2014
• 年：2014
• 卷：79
• 期：9
• 页码：4142-4147
• 全文大小：289K
• 年卷期：v.79,no.9(May 2, 2014)
• ISSN：1520-6904

文摘

A first example of 1,4-conjugate addition of 尾,纬-unsaturated N-sulfonylimines via the oxonium ylides trapping process was developed. This method afforded a novel and efficient access for the high regio- and diastereoselective construction of 伪-hydroxyl-未-amino esters derivatives, which exhibit inhibitory activity on PTP1B and SIRT1 enzymes in vitro. The synthetic potentials and the biological activity of the resulting products were well demonstrated to be promising for drug discovery.