反应详情

To a solution of 8-[3-(2,5-dioxo-2,5-dihydropyrrol-1-yl)propionylamino]octanoic acid (917 mg, crude) in dry THF (15 ml) was added TSTU (1.07 mg) and DIPEA (0.65 ml). The mixture was stirred under nitrogen over night. The mixture was concentrated. To the residue was added EtOAc and the precipitate was filtered off. The filtrate was extracted with 0.1 N HCl (2×) and brine (1×), dried (Na2SO4) and concentrated to give an off-white solid. Overall yield 37% (444 mg). LC-MS, M/z: 408.39 (M+1).

1. concentrationThe mixture was concentrated
2. additionTo the residue was added EtOAc
3. filtrationthe precipitate was filtered off
4. extractionThe filtrate was extracted with 0.1 N HCl (2×) and brine (1×)
5. dry with materialdried (Na2SO4)
6. concentrationconcentrated
7. customto give an off-white solid