Sodium Bicarbonate → HCID 24771917, compound

Participants

Reaction Steps

To a solution of the compound obtained in Example A4 (50 mg) and methylamine hydrochloride (8 mg) in methylene chloride (1 mL) were added 1-hydroxybenzotriazole monohydrate (23 mg), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (29 mg) and triethylamine (21 μL), and the mixture was stirred at room temperature overnight. To the reaction mixture were added methylene chloride and an aqueous saturated sodium hydrogencarbonate solution. After stirring vigorously for 10 minutes, the organic layer was separated and concentrated in vacuo. The resultant crude product was purified by column chromatography on silica gel (solvent; chloroform/methanol=100/0 to 95/5) and triturated to give 6-(2-chlorophenyl)-7-(4-chlorophenyl)-3-[N-[1-(N-methylcarbamoyl)cyclohexyl]-carbamoyl]pyrazolo[1,5-a]pyrimidine (25 mg; yield: 61%).

Provenance & Evidence