Water → HCID 178431642, compound

Participants

Reaction Steps

Under a nitrogen atmosphere, triethylamine (49.5 μl, 0.355 mmol) was added at 0° C. to a solution of the cis-4-[(4-methyl-1H-indazol-5-yl)oxy]cyclohexanamine hydrochloride (100 mg, 0.355 mmol) obtained in Example 410 in tetrahydrofuran (4 ml), followed by adding dropwise thereto a solution of methanesulfonyl chloride (28 μl, 0.362 mmol) in dichloromethane (2 ml). After 30 minutes, the resulting mixture was heated to room temperature and triethylamine (0.355 mmol) was further added thereto. After 2 hours, triethylamine (0.355 mmol) and methanesulfonyl chloride (0.355 mmol) were further added thereto. After 2 hours, the reaction solution was poured into water and extracted with ethyl acetate. The extract solution was concentrated under reduced pressure and the resulting residue was purified by a silica gel column chromatography (eluent: chloroform/ethyl acetate) to obtain cis-N-{4-[(4-methyl-1H-indazol-5-yl)oxy]cyclohexyl}methanesulfonamide (31.7 mg, 28%).

Provenance & Evidence