Diisopropylethylamine → HCID 51036182, compound

Participants

Reaction Steps

7-[[(7R)-8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-2-methyl-2,3-dihydrobenzofuran-4-carboxylic acid 30d (70 mg, 0.20 mmol), 1-methyl-piperidyl-4-yl-amine (23 mg, 0.20 mmol), O-(benzotriazol-1-yl)-N,N,N′,N′-tetra methyluronium tetrafluoroborate (64 mg, 0.20 mmol) and diisopropylethylamine (65 mg, 0.50 mmol) were dissolved in 30 mL of dichloromethane. The reaction solution was stirred for 2 hours. The resulting solution was added with 20 mL of saturated sodium bicarbonate solution and extracted with dichloromethane (50 mL×3). The combined organic phase was washed with water (30 mL) and saturated sodium chloride solution (30 mL) successively, then dried over anhydrous magnesium sulfate, filtered and the filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography to obtain the title compound 7-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-2-methyl-N-(1-methyl-4-piperidyl)-2,3-dihydrobenzofuran-4-carboxamide 30 (40 mg, yield: 36.0%) as a white solid.

Provenance & Evidence