The ubiquitous presence of the indole fragment in natural products and drugs asks for ever novel syntheses. We report an unprecedented mild, two-step synthesis of 2-tetrazolo substituted indoles based on the Ugi-tetrazole reaction combined with an acidic ring closure. A gram-scale synthesis, a bioactive compound and further transformations were performed.
X. Lei, P. Lampiri, P. Patil, G. Angeli, C. G. Neochoritis and A. Dömling, Chem. Commun., 2021, 57, 6652 DOI: 10.1039/D1CC02384E
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