反应详情

A solution of (S)-2-((tert-butoxycarbonyl)amino)-8-oxodecanoic acid (0.76 mmol, 1 eq; prepared as described in J. Med. Chem. 2008, 51(8), pp 2350-2353), EDC.HCl (1 eq), HOBT (1 eq) in DMF (0.2 M) was stirred at room temperature for 10 min. 3-(2-aminoacetyl)-1-methylquinolin-2(1 H)-one (1.1 eq) in DMF (3 eq) was subsequently added, followed by DIPEA (2.2 eq) and the mixture was stirred at room temperature for 2 h. The mixture was diluted with DCM and washed with brine. The organic phase was dried (Na2SO4), filtered and concentrated. The residue was purified by flash chromatography (SiO2, Petroleum ether/EtOAc, from 10% EtOAc to 80% EtOAc), to give the title compound as an oil. MS (ES) C27H37N3O6 requires: 499.60, found: 500.

1. washwashed with brine
2. dry with materialThe organic phase was dried (Na2SO4)
3. filtrationfiltered
4. concentrationconcentrated
5. customThe residue was purified by flash chromatography (SiO2, Petroleum ether/EtOAc, from 10% EtOAc to 80% EtOAc)