反应详情

温度

100 °C

A reaction mixture of 5-Bromo-quinoline-8-carboxylic acid methyl ester (600.00 mg; 2.25 mmol; 1.00 eq.), N—[(S)-2-Amino-2-(3-fluoro-phenyl)-ethyl]-N-methyl-4-nitro-benzenesulfonamide (876.48 mg; 2.48 mmol; 1.10 eq.), potassium phosphate, tribasic (957.26 mg; 4.51 mmol; 2.00 eq.), dicyclohexyl-(2′,4′,6′-triisopropyl-biphenyl-2-yl)-phosphane (214.99 mg; 0.45 mmol; 0.20 eq.), palladium (+2) acetate (50.62 mg; 0.23 mmol; 0.10 eq.) and toluene (5 ml) in microwave tube were stirred at 100° C. overnight. The crude was purified by prep HPLC (Basic condition) to afford (S)-5-{1-(3-Fluoro-phenyl)-2-[methyl-(4-nitro-benzenesulfonyl)-amino]-ethylamino}-quinoline-8-carboxylic acid methyl ester (250 mg). LC-MS (M+H=339, obsd.=339).

1. customThe crude was purified by prep HPLC (Basic condition)