反应详情

N-Cyclopropyl-3-fluoro-5-[3-[[1-(2-hydroxyphenyl)cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-4-methyl-benzamide (Preparation 1k, 5 g), 1-bromo-2-chloroethane (9.58 mL) and cesium carbonate (37.5 g) were stirred together in acetonitrile (200 mL) at 80° C. under nitrogen for 16 h. The cooled reaction mixture was evaporated to dryness, diluted with water (500 mL) and extracted with dichloromethane (3×300 mL). The combined organics were dried (MgSO4), filtered and evaporated. The residue was triturated with 1:1 iso-hexane:diethyl ether to give the subtitle compound (4.60 g).

1. customThe cooled reaction mixture
2. customwas evaporated to dryness
3. additiondiluted with water (500 mL)
4. extractionextracted with dichloromethane (3×300 mL)
5. dry with materialThe combined organics were dried (MgSO4)
6. filtrationfiltered
7. customevaporated
8. customThe residue was triturated with 1:1 iso-hexane