反应详情

A mixture of methyl 3-hydroxy-5-[(3S)-1-methyl-2-oxo-pyrrolidin-3-yl]oxy-benzoate (Intermediate 8) (530 mg, 2 mmol), 5-chloro-N,N-dimethyl-pyrazine-2-carboxamide (CAS no. 915949-00-7) (446 mg, 2.4 mmol) and potassium carbonate (552 mg, 4 mmol) in acetonitrile (15 mL) was stirred at 120° C. for 2 hours. The mixture was evaporated and the residue dissolved in ethyl acetate (30 mL), washed with water (2×10 mL) and brine (20 mL), dried (MgSO4) and evaporated. The residue was purified by flash chromatography on silica eluting with 50 to 100% ethyl acetate in isohexane to afford the product (772 mg, 93%). m/z 415 (M+H+).

1. customThe mixture was evaporated
2. dissolutionthe residue dissolved in ethyl acetate (30 mL)
3. washwashed with water (2×10 mL) and brine (20 mL)
4. dry with materialdried (MgSO4)
5. customevaporated
6. customThe residue was purified by flash chromatography on silica eluting with 50 to 100% ethyl acetate in isohexane