反应详情

5-(2-Oxo-pyrrolidin-1-yl)-isophthalic acid monomethyl ester (D63) (1.0 g, 3.8 mmol) was dissolved in DMF (7 ml) and treated with N-methyl propylamine (0.42 g, 5.7 mmol), HOBt (0.62 g, 4.56 mmol) and EDC (1.02 g, 5.32 mmol) and the resulting solution was stirred overnight at room temperature. It was then evaporated to dryness and the residue was partitioned between EtOAc and dil.HCl. The organic phase was separated, washed with dil.HCl (×2), dil.NaHCO3 (×3) and brine (×1). It was dried (MgSO4) and evaporated to leave the crude product which was purified by silica chromatography eluting with DCM/MeOH to afford the pure title compound (D64) (0.40 g, 33%).

1. customIt was then evaporated to dryness
2. customthe residue was partitioned between EtOAc
3. customThe organic phase was separated
4. washwashed with dil
5. dry with materialIt was dried (MgSO4)
6. customevaporated
7. customto leave the crude product which
8. customwas purified by silica chromatography
9. washeluting with DCM/MeOH