反应详情

温度

85 °C

Combine (R)-5-chloro-3-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-6-fluoro-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione (0.050 g, 0.15 mmol) and 2-fluoro-4-iodoaniline (0.052 g, 0.22 mmol) in de-gassed dioxane (2.0 mL). Add palladium acetate (1.6 mg) and Xantphos (8.5 mg) and sodium t-butoxide (35 mg). Heat to 85° C. After 2 hours, dilute with ethyl acetate, wash with aqueous hydrochloric acid and then brine, dry over sodium sulfate, and concentrate in vacuo to give a residue. Purify the residue with flash chromatography eluting with ethyl acetate/hexane to give the title compound.

1. washwash with aqueous hydrochloric acid
2. dry with materialbrine, dry over sodium sulfate
3. concentrationconcentrate in vacuo
4. customto give a residue
5. customPurify the residue with flash chromatography
6. washeluting with ethyl acetate/hexane