反应详情

A solution of N-(2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)-3-chloro-2,4-difluoro-N-methylbenzamide (647 mg, 1.78 mmol) in acetonitrile (10 mL) was heated with potassium carbonate (492 mg, 3.56 mmol) and methyl 3-hydroxy-5-[(3S)-tetrahydrofuran-3-yloxy]benzoate (424 mg, 1.78 mmol) at 160° C. for 2.5 hours in a microwave reactor. Water (15 mL) and ethyl acetate (20 mL) was added to the reaction mixture, the layers separated and the aqueous phase extracted with ethyl acetate (3×20 mL). The combined organic extract was washed with brine (10 mL) and dried (MgSO4), filtered and evaporated to a residue which was chromatographed on silica, eluting with 40-100% ethyl acetate in isohexane, to give the desired compound as a clear oil (200 mg).

1. customthe layers separated
2. extractionthe aqueous phase extracted with ethyl acetate (3×20 mL)
3. extractionThe combined organic extract
4. washwas washed with brine (10 mL)
5. dry with materialdried (MgSO4)
6. filtrationfiltered
7. customevaporated to a residue which
8. customwas chromatographed on silica
9. washeluting with 40-100% ethyl acetate in isohexane