One-pot synthesis of 2,3-difunctionalized indoles via Rh(iii)-catalyzed carbenoid insertion C-H
Honggui Lv1, Jingjing Shi, Bo Wu
1Key Laboratory of Molecular Clinical Pharmacology & Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou, Guangdong 511436, P. R. China. yiwei@gzhmu.edu.cn yiwei.simm@simm.ac.cn.
Abstract:
Reported herein is the first Rh(iii)-catalyzed carbenoid insertion C-H activation/cyclization of N-arylureas and α-diazo β-keto esters. The redox-neutral reaction has the following features: good to excellent yields, broad substrate/functional group tolerance, exclusive regioselectivity, and no need for additional oxidants or additives, which render this methodology as a more efficient and versatile alternative to the existing methods for the synthesis of 2,3-difunctionalized indoles.
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