反应详情

A mixture of 5-tert-butyl-3-butylthiazol-2(3H)-imine (free base of Example 6A, 500 mg, 2.4 mmol), 5-chloro-2-fluorobenzoic acid (670 mg, 2.8 mmol), EDCI (900 mg, 4.7 mmol), HOBt (635 mg, 4.7 mmol) and DMAP (36 mg, 0.3 mmol) in pyridine (20 mL) was stirred at room temperature for 2 hours. The solvent was removed, the mixture was diluted with water, and extracted with EtOAc. The organic extract was dried (Na2SO4), filtered and concentrated. The residue was triturated with EtOAc, to give 537 mg (61%) of the title compound. MS (ESI) m/z 369 (M+H)+.

1. customThe solvent was removed
2. additionthe mixture was diluted with water
3. extractionextracted with EtOAc
4. extractionThe organic extract
5. dry with materialwas dried (Na2SO4)
6. filtrationfiltered
7. concentrationconcentrated
8. customThe residue was triturated with EtOAc