1-Hydroxybenzotriazole → Methyl cis(+/-)-3-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate

Participants

Reaction Steps

The same operation as in Example (1g) was performed using methyl cis(±)-3-(4-amino-3-methoxypiperidin-1-yl)-5-fluorobenzoate obtained in Example (175b) (50.6 mg, 0.18 mmol), 4-chloro-5-ethyl-1H-imidazole-2-carboxylic acid obtained by the method described in Example (1d) (28 mg, 0.16 mmol), WSC hydrochloride (93.7 mg, 0.49 mmol) and HOBt (22 mg, 0.16 mmol), to obtain 56 mg of the title compound as a pale yellow solid (78%).

Provenance & Evidence