反应详情

TBTU (138 mg, 0.43 mmol) was added to a stirred solution of 8-(1-(3-fluorophenyl)pyrrolidin-2-yl)-2-((R)-2-methylmorpholino)-4-oxo-4H-chromene-6-carboxylic acid (97 mg, 0.21 mmol), DIPEA (0.075 mL, 0.43 mmol) dissolved in DMF (1.5 mL) under nitrogen. The resulting solution was stirred at room temperature for 1.5 h. Morpholine (0.028 mL, 0.32 mmol) was added and the reaction mixture was stirred at room temperature for 1 h. The reaction mixture was purified by preparative HPLC. The fractions were evaporated to dryness, the residue was dissolved in DCM, dried over MgSO4 and evaporated to dryness to afford 8-(1-(3-fluorophenyl)pyrrolidin-2-yl)-2-((R)-2-methylmorpholino)-6-(morpholine-4-carbonyl)-4H-chromen-4-one (63 mg, 56%) as a yellow foam.

1. stirringthe reaction mixture was stirred at room temperature for 1 h
2. customThe reaction mixture was purified by preparative HPLC
3. customThe fractions were evaporated to dryness
4. dissolutionthe residue was dissolved in DCM
5. dry with materialdried over MgSO4
6. customevaporated to dryness