Diisopropylcarbodiimide → Ethyl-2-(2-chloro-5-{[(tert-butoxycarbonyl)-amino]-methyl}-phenylamino)-6-(2,2-difluoro-ethoxy)-1-methyl-1H-benzimidazole-5-carboxylate

Participants

Reaction Steps

A mixture of tert-butyl 4-chloro-3-isothiocyanatobenzylcarbamate ((see Example 2, step (c)) 974 mg; 3.26 mmol) and ethyl 5-amino-2-(2,2-difluoroethoxy)-4-(methylamino)benzoate ((see Example 59, step (g)) 894 mg; 3.26 mmol) in DMF (10 mL) was stirred over night at rt. DIC (411 mg; 3.26 mmol) was added and the mixture was heated at 90° C. for 1.5 h. The mixture was concentrated and the residue was recrystallized from EtOAc/petroleum ether and washed with Et2O to give the sub-title compound. Yield: 1.75 g (99%).

Provenance & Evidence