反应详情

To a solution of compound prepared in example 8 (250 mg, 0.454 mmoles) in DMF (2 mL), (tetrahydro-2H-pyran-4-yl)methanamine hydrochloride (83 mg, 0.545 mmoles), HOBT (Catalyst), EDC.HCl (130 mg, 0.681 mmoles) and N-ethyl morpholine (0.173 ml, 1.362 mmoles) were added and the reaction mixture was srirred at 25° C. for 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 purified by column chromatography to yield 200 mg (68%) of product as white solid.

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