4-Methylmorpholine → 2-[(3,5-Dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[2-(trifluoromethyl)benzyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide

Participants

Reaction Steps

The title compound was prepared following the procedure as described for Example-1 using 2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxylic acid (Intermediate-3, 0.050 g, 0.127 mmol), O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate (0.082 g, 0.255 mmol), N-methyl morpholine (0.5 mL), DMF (1.0 mL), THF (5.0 mL) and 1-[2-(trifluoromethyl)phenyl]methanamine (Intermediate-4, 0.027 g, 0.154 mmol) to afford 0.015 g of the desired product. 1HNMR (DMSO-d6): δ 1.21 (s, 3H), 1.48 (s, 3H), 3.01 (s, 2H), 4.68 (m, 2H), 7.19 (s, 1H), 7.46-7.51 (m, 2H), 7.62 (d, J=7.8 Hz, 1H), 7.72 (d, J=7.8 Hz, 1H), 8.27 (m, 1H), 8.41 (s, 2H), 10.89 (s, 1H), 11.42 (s, 1H); MS [M+H]+: 550.31.

Provenance & Evidence