Affiliation:
1. Jiangxi Province Key Laboratory of Synthetic Pharmaceutical Chemistry College of Chemistry &Chemical Engineering Gannan Normal University Shida South Road 34100 Ganzhou P. R. China
2. Key Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Diseases of Ministry of Education School of Pharmaceutical Sciences of Gannan Medical University Ganzhou 341000 P. R. China
Abstract
AbstractPolycyclic indoles are prevailed in natural products, pharmaceuticals and biologically active compounds. Herein is described photo‐induced difluoromethylation‐cyclization of N‐alkene tethered indoles to synthesis of tetrahydropyrido[1,2‐a]indole using 5‐((difluoromethyl)sulfonyl)‐1‐phenyl‐1H‐tetrazole as a CF2H radical source. This photochemical reaction tolerates an array of functional groups like ester, cyano, ketone, halide, ether, aldehyde and heteocycles. Mechanistic experiments indicated that the difluoromethyl radical and the single electron transfer were involved.
Funder
National Natural Science Foundation of China
Foundation of Jiangxi Educational Commission