Copper-Catalyzed Dearomative [3 + 2] Annulation of Indoles with 2-Iodoacetic Acid
Ren-Xiao Liang1, Hu-Jie Cai1, Ming-Hua Mao1
1College of Chemical Engineering, State Key Laboratory Breeding Base of Green-Chemical Synthesis Technology, Zhejiang University of Technology, Chaowang Road 18#, Hangzhou 310014, China.
Abstract:
An efficient copper-catalyzed dearomative [3 + 2] annulation of indoles with 2-iodoacetic acid is developed. By employing Cu(OTf)2/2,2'-bis(2-oxazoline) as the catalyst and LPO as the oxidant, a series of indoline-fused butyrolactones were synthesized in moderate to good yields. The reaction features mild conditions, a broad substrate scope, and readily available starting materials. Furthermore, synthetic transformations of the products were conducted to demonstrate the practical utility of this reaction.
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