反应详情

To a solution of the product from the previous step (1.4 g) in DMAC was added DIPEA (2 eq) followed by 5-(4-fluorophenyl)-2-methylthiazole-4-carboxylic acid (2.3 g) and HATU (1.1 eq). The reaction was allowed to stir at rt for 15 h, and was then concentrated in vacuo to remove the DMAC. The crude residue was taken up in EtOAc and washed with 1 M HCl, sat aq. NaHCO3, brine, dried (MgSO4), and concentrated. The crude residue was purified by chromatography on silica gel (EtOAc/hex) to give the title compound as a brown oil which crystallized (2.6 g). MS (ESI) 349.4 (M+H).

1. concentrationwas then concentrated in vacuo
2. customto remove the DMAC
3. washwashed with 1 M HCl
4. dry with materialdried (MgSO4)
5. concentrationconcentrated
6. customThe crude residue was purified by chromatography on silica gel (EtOAc/hex)