反应详情

温度

90 °C

4-Chloro-6-(5-chloro-2-fluoro-phenyl)-3-methyl-isoxazolo[5,4-d]pyrimidine (Prepared by method used for 0043) (298 mg, 1 mmole) was dissolved in dioxane (4 ml), added BINAP (4.67 mg, 0.0075), 4-Amino-nicotinic acid methyl ester (182 mg, 1.2 mmole), cesium carbonate (456 mg, 1.4 mmole), and Pd2(dba)3 (2.29 mg, 0.0025 mmole) to the mixture and heated to 90° C. overnight. Removed dioxane under vacuum and triturated residue with ethyl acetate (5 ml) and isolated product by filtration. Obtained 525 mg solid which also contained cesium carbonate as byproduct.

1. customRemoved dioxane under vacuum and triturated residue with ethyl acetate (5 ml)
2. customisolated product
3. filtrationby filtration