pntd.0009196.g002.tif (111.19 kB)
Synthesis of 2-aminobenzimidazoles.
figure
posted on 2021-02-22, 18:36 authored by Rafael Augusto Alves Ferreira, Celso de Oliveira Rezende Junior, Pablo David Grigol Martinez, Paul John Koovits, Bruna Miranda Soares, Leonardo L. G. Ferreira, Simone Michelan-Duarte, Rafael Consolin Chelucci, Adriano D. Andricopulo, Mariana K. Galuppo, Silvia R. B. Uliana, An Matheeussen, Guy Caljon, Louis Maes, Simon Campbell, Jadel M. Kratz, Charles E. Mowbray, Luiz Carlos DiasReagents and conditions: a) alkylamine, K2CO3, KF, DMF, 0°C—r.t.; b) NH3 (7.0 mol.L-1 in MeOH), 80°C, 1h, microwave; c) Aldehyde, NaBH(OAc)3, TFA or DCM, 0°C-r.t, 3h; d) H2 (1 bar), Pd/C, EtOAc/MeOH, r.t.; e) BrCN (1M in DCM), MeOH, 60°C; f) EDC, HOBt, DMF, r.t.. Detailed synthetic schemes are shown in S1 Information.
