Construction of 2-alkynyl aza-spiro[4,5]indole scaffolds via sequential C-H activations for modular click chemistry
Jun Zhang1, Mengmeng Wang, Huiying Wang
1School of Pharmaceutical Science, Shanxi Medical University, 56 Xinjian South Road, Taiyuan 030001, China. shurongban@sxmu.edu.cn.
Abstract:
Herein, we have developed a strategy of sequential C-H activations of indole to construct novel 2-alkynyl aza-spiro[4,5]indole scaffolds, which incorporated both alkyne and spiro-units into indole. Gram-scale synthesis and a one-pot, three-step synthesis demonstrated the utility of this protocol. Hybrid conjugates with an oseltamivir derivative further offered a powerful tool for the construction of a versatile spiroindole-containing library via click chemistry.
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