3-Aminopropionitrile → cis(+/-)-2-(4-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-N-(2-cyanoethyl)-4-methyl-1,3-thiazole-5-carboxylic acid amide

Participants

Reaction Steps

The same operation as in Example (1g) was performed using cis(±)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid obtained in Example (14a) (75 mg, 0.18 mmol), 3-aminopropionitrile (14 mg, 0.20 mmol), WSC hydrochloride (111 mg, 0.58 mmol), HOBT (39 mg, 0.29 mmol), dichloromethane (1.5 mL) and DMA (1.5 mL), to obtain 69 mg of the title compound as a white solid (82%).

Provenance & Evidence