反应详情

To solution of 2-[2-(2,4-dichloro-phenoxy)-acetylamino]-isonicotinic acid (16 mg, 0.047 mmol), furfuryl amine (9.1 mg, 0.094 mmol) and DMAP (8.6 mg, 0.07 mmol) in DMF 4 ml was added PyBOP (36 mg, 0.07 mmol) at room temperature, and stirred. Reaction mixture was poured onto ice cold water, diluted by methanol/MC mixture (10%). The organic phase was separated, sequentially washed with aqueous sodium bicarbonate, brine and water, dried over anhydrous MgSO4, and concentrated. The resultant crude product was purified by PLC (MeOH:MC=1:9) to afford 2-[2-(2,4-dichloro-phenoxy)-acetylamino]-N-furan-2-ylmethyl-isonicotinamide as a colorless solid (5 mg, 25.3% yield).

1. customReaction mixture
2. additionwas poured onto ice cold water
3. customThe organic phase was separated
4. washsequentially washed with aqueous sodium bicarbonate, brine and water
5. dry with materialdried over anhydrous MgSO4
6. concentrationconcentrated
7. customThe resultant crude product was purified by PLC (MeOH:MC=1:9)