1-Hydroxybenzotriazole → HCID 58011937, compound

Participants

Reaction Steps

70.0 mg (0.238 mmol) of [3-(4-chlorophenyl)-4-cyclopropyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]-acetic acid from Example 88A and 53.3 mg (0.262 mmol) of 1-methyl-1-[(3-trifluoromethyl)-phenyl]ethylamine from Example 1A are placed in 2 ml of dimethylformamide and treated with 38.6 mg (0.286 mmol) of HOBt. After 10 mins' stirring, 59.4 mg (0.310 mmol) of EDC hydrochloride are added and the mixture is stirred overnight at room temperature. For the workup, the reaction mixture is partitioned between dichloromethane and water, and the organic phase is separated, dried over sodium sulphate and concentrated. The residue is purified by flash chromatography on silica gel (eluent: dichloromethane/methanol first 200:1, then 100:1). 97 mg (85% of theory) of the target compound are thus obtained.

Provenance & Evidence