Synthesis of Enantioenriched Indole-Fused Rings through Asymmetric (4+3) Cycloadditions of Indolyldimethanols with
Shao-Chuan Li1, Xue Tian2, Zhifei Zhao2
1Anhui Provincial Key Laboratory of Green Carbon Chemistry, School of Chemistry & Materials Engineering, Fuyang Normal University, Fuyang 236037, PR China.
Abstract:
We developed an efficient and operationally simple chiral phosphoric acid-catalyzed method for the straightforward synthesis of enantioenriched indole-fused azepane derivatives via the reaction of indolyldimethanols with 5-aminopyrazoles. A wide variety of enantioenriched indole-fused ring products were obtained in good yields with excellent enantioselectivities under mild conditions. In addition, a scale-up experiment and the synthetic transformations of the cycloadducts further highlighted their synthetic utility.
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