反应详情

温度

80 °C

(1R,2R) and (1S,2S)-2-(4-chlorophenyl)-5′-fluoro-2-isopropylspiro[cyclopropane-1,3′-indolin]-2′-one prepared according to Scheme 2 (0.33 g, 1 mmol), and the 3-bromo-5-iodo-benzoic acid methyl ester (0.409 g, 1.2 mmol), CuI (20 mg), K2CO3 (0.276 g, 2 mmol) were placed in a Schlenk tube under argon atmosphere and dissolved in dry acetonitrile. The N,N′-dimethyl-1,2-ethanediamine (21 μL) was added into the mixture. The mixture was stirred at 80° C. for 14 hours. The solvent was removed in vacuo and the residue was purified by flash column chromatography to give the title compound as white powder (0.444 g, 82%). LC/MS m/e calcd. for C27H22BrClFNO3: 541, observed (M+H)+: 542.

1. customThe solvent was removed in vacuo
2. customthe residue was purified by flash column chromatography