反应详情

A mixture of 5-bromo-3-(6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazin-2-ylamino)-1-methylpyridin-2(1H)-one 110c (500 mg, 1.54 mmol), (2-{6-oxo-8-thia-5-azatricyclo-[7.4.0.02,7]trideca-1(9),2(7)-dien-5-yl}-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methyl acetate 111a (750 mg, 1.56 mmol), PdCl2(dppf) (170 mg, 0.23 mmol), K3PO4 (150 mg), and sodium acetate (60 mg) in MeCN (25 mL) and water (5 mL) was heated at reflux for 2 h. The solvent was evaporated in vacuo and the residue was purified on reverse phase Combi-flash to give 169a (369 mg, 40%). MS: [M+H]+ 600.

1. temperaturewas heated
2. temperatureat reflux for 2 h
3. customThe solvent was evaporated in vacuo
4. customthe residue was purified on reverse phase Combi-flash