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Please login or sign up for a free trial to access the full content. Variation 4: Introduction of Aryl Groups

DOI: 10.1055/sos-SD-110-00001

Joule, J. A.Science of Synthesis Knowledge Updates, (20102339.

N-Arylation of an indole with fluoroarenes carrying electron-withdrawing groups is efficient using potassium fluoride/alumina and a catalytic quantity of 18-crown-6 in dimethyl sulfoxide at 120°C,[‌1439‌] or with microwave heating at 180°C,[‌1440‌] and N-4-pyridylation of 3-(4-fluorophenyl)-1H-indoles 1172 giving 1173 is achieved using 4-bromopyridine in the presence of copper(I) bromide and potassium carbonate (Scheme 488).[‌145‌]

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