Potassium Carbonate → acetic acid 2-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-6-{8-[4-(morpholine-4-carbonyl)-phenylamino]-imidazo[1,2-a]pyrazin-6-yl}-benzyl ester

Participants

Reaction Steps

A solution of acetic acid 2-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-6-(4,4,5,5-tetramethyl[1,3,2]dioxaborolan-2-yl)-benzyl ester (491.3 mg, 1 mmol), [4-(6-bromo-imidazo[1,2-a]pyrazin-8-ylamino)-phenyl]-morpholin-4-yl-methanone (200 mg, 0.5 mmol), K2CO3 (137 mg, 1 mmol), Pd2(dba)3 (45.4 mg, 0.05 mmol) and X-Phos (94.5 mg, 0.2 mmol) in 30 mL dioxane and 10 mL water was stirred at 90° C. overnight. The crude reaction mixture was filtered. The filtrate was evaporated and the resulting residue was purified through a silica-gel column (ethyl acetate:petroleum ether=1:2) to give compound the desired product as a yellow oil (320 mg, 93% yield).

Provenance & Evidence