1-Hydroxybenzotriazole → cis(+/-)-4-Chloro-N-{3-(2,2-difluoroethoxy)-1-(trifluoroacetyl)piperidin-4-yl}-5-ethyl-1H-imidazole-2-carboxamide

Participants

Reaction Steps

The same operation as in Example (106d) was performed using cis(±)-3-(2,2-difluoroethoxy)-1-(trifluoroacetyl)piperidin-4-amine obtained in Example (121e) (0.79 g, 2.86 mmol), 4-chloro-5-ethyl-1H-imidazole 2-carboxylic acid (85% content, 0.62 g, 3 mmol), WSC hydrochloride (1.15 g, 6 mmol), HOBt (0.61 g, 4.5 mmol), DMA (15 mL) and dichloromethane (15 mL). The resulting residue was purified by silica gel column chromatography (elution solvent: ethyl acetate/hexane=1/4, 2/3, 3/2, 4/1) to obtain 0.82 g of the title compound as a colorless amorphous solid (63%).

Provenance & Evidence