反应详情

N-(4-Fluorophenyl)-N′-[4-(2-aminopyridin-4-yloxy)-2-fluorophenyl]malonamide (21.3 mg) was dissolved in N,N-dimethylformamide (0.5 ml), and then triethylamine (0.030 ml) and cyclopropanecarbonyl chloride (0.010 ml) were added dropwise thereto under a nitrogen atmosphere at room temperature, followed by stirring for 1 hr. To the reaction mixture were added a 1 N aqueous solution of sodium hydroxide (1.0 ml) and methanol (1.0 ml), followed by stirring and extracting with ethyl acetate. The organic layer was concentrated under a reduced pressure to give a residue, which was purified by silica gel column chromatography (FUJI Silysia NH, eluent; ethyl acetate). Fractions containing the target compound were concentrated to give a residue, which was then dried in vacuum to provide the titled compound (9.6 mg, 39%) as white powder.

1. customat room temperature
2. stirringby stirring
3. extractionextracting with ethyl acetate
4. concentrationThe organic layer was concentrated under a reduced pressure
5. customto give a residue, which
6. customwas purified by silica gel column chromatography (FUJI Silysia NH, eluent; ethyl acetate)
7. additionFractions containing the target compound
8. concentrationwere concentrated
9. customto give a residue, which
10. customwas then dried in vacuum