反应详情

7-[[(7R)-8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-2,3-dihydrobenzofuran-4-carboxylic acid 1q (276 mg, 0.63 mmol) and O-(benzotriazol-1-yl)-N,N,N′,N′-tetra methyluronium tetrafluoroborate (202 mg, 0.63 mmol) were dissolved in 20 mL of anhydrous dichloromethane, added with diisopropylethylamine (0.2 mL, 1.4 mmol), [(2R)-4-benzylmorpholin-2-yl]methanamine 15a (130 mg, 0.63 mmol) successively with stirring. The reaction solution was stirred for 3 hours. The resulting solution was added with 10 mL saturated sodium carbonate solution and 10 mL of dichloromethane successively, and seperated. The organic phase was washed with sodium carbonate solution (50 mL×2), water (50 mL) and saturated sodium chloride solution (50 mL) successively, then dried over anhydrous sodium 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 N-[[(2R)-4-benzylmorpholin-2-yl]methyl]-7-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-2,3-dihydrobenzofuran-4-carboxamide 15b (370 mg, yield: 94.0%) as a white solid.

1. stirringThe reaction solution was stirred for 3 hours
2. customseperated
3. washThe organic phase was washed with sodium carbonate solution (50 mL×2), water (50 mL) and saturated sodium chloride solution (50 mL) successively
4. dry with materialdried over anhydrous sodium sulfate
5. filtrationfiltered
6. concentrationthe filtrate was concentrated under reduced pressure
7. customThe resulting residue was purified by silica gel column chromatography