反应详情

5-({[(2,6-dichlorophenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acid (51 mg, 0.14 mmol) was dissolved in DMF (1 mL) and CDI (34 mg, 0.21 mmol) was added. The mixture was stirred until acid activation was complete. 1-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-N-methylmethanamine.HCl (32 mg, 0.14 mmol) and DIPEA (0.074 mL, 0.42 mmol) were sonicated in DMF (0.5 mL) for 15 min. 0.5 mL of activated acid solution was added to 0.25 mL of amine solution and the reaction was stirred at ambient temperature for 18 h, then microwaved (120° C., 200 W) for 2×20 min. The reaction was concentrated, dissolved in DCM and washed with water (3×1.5 mL) and saturated brine (1 mL)). The organic layer was dried over MgSO4 and solvents were removed in vacuo. A portion of the crude product was purified using prep method A.

1. stirringthe reaction was stirred at ambient temperature for 18 h
2. custommicrowaved (120° C., 200 W) for 2×20 min
3. concentrationThe reaction was concentrated
4. dissolutiondissolved in DCM
5. washwashed with water (3×1.5 mL) and saturated brine (1 mL))
6. dry with materialThe organic layer was dried over MgSO4 and solvents
7. customwere removed in vacuo
8. customA portion of the crude product was purified