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

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Reaction Steps

A mixture of ethyl 5-amino-2-(2,2-difluoroethoxy)-4-(methylamino)benzoate (0.737 g; 2.68 mmol; crude material from step (g)) and N-(4-chloro-3-isothiocyanatobenzyl)-1-(trifluoromethyl)cyclopropane carboxamide (0.900 g; 2.68 mmol) in THF (100 mL) was stirred over night at rt. DIC (0.338 g; 2.68 mmol) was added and the mixture was stirred for 6 h at rt. Another portion of DIC (0.169 g; 1.34 mmol) was added and the mixture stirred for another 6 h at rt. The mixture was concentrated and purified by column chromatography to give the sub-title compound. Yield: 0.790 g (51%).

Provenance & Evidence