反应详情

To a solution of compound prepared in example 6 (250 mg, 0.60 mmoles) in DMF (2 mL), (tetrahydro-2H-pyran-4-yl)methanamine (138 mg, 1.20 mmoles), HOBT (121 mg, 0.90 mmoles), EDC.HCl (138 mg, 0.72 mmoles) and N-ethyl morpholine (227 μL, 1.80 mmoles) were added and reaction mixture was srirred at 25° C. for 2-5 hours under nitrogen atmosphere. The reaction mixture was poured into ice cold water and extracted with ethyl acetate. The combined ethyl acetate extract was washed with water & brine, dried over sodium sulphate and evaporated under reduced pressure. The crude product was triturated with hexane to yield 180 mg (49%) of product as white solid.

1. customreaction mixture
2. additionThe reaction mixture was poured into ice cold water
3. extractionextracted with ethyl acetate
4. extractionThe combined ethyl acetate extract
5. washwas washed with water & brine
6. dry with materialdried over sodium sulphate
7. customevaporated under reduced pressure
8. customThe crude product was triturated with hexane