反应详情

温度

145 °C

tert-butyl 6-chloropyridazin-3-yl((1-(3-fluoropyridin-2-yl)cyclobutyl)methyl)carbamate (500 mg, 1.27 mmol), ethyl thiazole-5-carboxylate (300 mg, 1.91 mmol), Pd(OAc)2 (86 mg, 0.13 mmol), JohnPhos (92 mg, 0.26 mmol) and Cs2CO3 (827 mg, 2.54 mmol) in toluene (10 mL) were combined and heated in a microwave reactor for 30 min at 145° C. The reaction mixture was filtered through a celite plug and the filtrate was concentrated. The resulting residue was purified on silica gel using a mixture of ethyl acetate and hexanes to provide the title compound as yellow oil (162 mg, 82% pure, 21%), LRMS (M+H+) m/z 514.3.

1. filtrationThe reaction mixture was filtered through a celite plug
2. concentrationthe filtrate was concentrated
3. customThe resulting residue was purified on silica gel using
4. additiona mixture of ethyl acetate and hexanes