反应详情

To tert-butyl 4-(2-(1-(3,3-diphenylpropyl)-3-(4-(4-(methylsulfonamido)phenyl)thiazol-2-yl)ureido)ethyl)piperidine-1-carboxylate (0.35 g, 0.49 mmol) in DMF (10 ml) was added NCS (0.065 g, 0.49 mmol). The resulting mixture was stirred overnight at room temperature. After this time the mixture was concentrated under reduced pressure and the residue partitioned between ethyl acetate and sat. aq. NaHCO3. The organic layer was washed with water and brine, dried over MgSO4 and concentrated under reduced pressure to give the crude product as a thick yellow oil. This crude product was purified by combi-flash (10-50% EtOAc/hexane). To give tert-butyl 4-(2-(3-(5-chloro-4-(4-(methylsulfonamido)phenyl)thiazol-2-yl)-1-(3,3-diphenylpropyl)ureido)ethyl)piperidine-1-carboxylate 50 as a yellow oil.

1. concentrationAfter this time the mixture was concentrated under reduced pressure
2. customthe residue partitioned between ethyl acetate and sat. aq. NaHCO3
3. washThe organic layer was washed with water and brine
4. dry with materialdried over MgSO4
5. concentrationconcentrated under reduced pressure
6. customto give the crude product as a thick yellow oil
7. customThis crude product was purified by combi-flash (10-50% EtOAc/hexane)