1-Hydroxybenzotriazole → HCID 67350091, compound

Participants

Reaction Steps

(S)-2-[3-(9-Methylthio-6-oxo-2,3,3a,4-tetrahydro-1H,6H-5,8,10,10b-tetraazabenzo[e]azulen-5-yl)phenyl]-1,3-oxazole-4-carboxylic acid (300 mg, 0.685 mmol) obtained in Step 1 of Example 124 was dissolved in DMF (7 mL), and the mixture was stirred at room temperature for 2 hours after adding 28% ammonia water (0.0830 mL, 1.37 mmol), 1-ethyl-3-(3dimethylaminopropyl)carbodiimide hydrochloride (263 mg, 1.37 mmol), and 1-hydroxybenzotriazole.monohydrate (210 mg, 1.37 mmol). Thereafter, ethyl acetate was added to the mixture, and the mixture was washed with water and saturated brine. The organic layer was dried over anhydrous magnesium sulfate, and the residue obtained upon concentration under reduced pressure was then purified by silica gel column chromatography to give (S)-2-[3-(9-methylthio-6-oxo-2,3,3a,4-tetrahydro-1H,6H-5,8,10,10b-tetraazabenzo[e]azulen-5-yl)phenyl]-1,3-oxazole-4-carboxamide (261 mg, 87%).

Provenance & Evidence