反应详情

A mixture of (5-fluoro-2-methylindol-1-yl)acetic acid methyl ester (0.2 g), 4-benzenesulfonylthiazole-5-carbaldehyde (0.23 g) and 1,2-dichloroethane (7.0 mL) at 0° C. was treated dropwise with a mixture of triethylsilane (2.2 mL), trifluoroacetic acid (0.6 mL) and 1,2-dichloroethane (2.0 mL), and the resulting mixture was stirred at room temperature overnight. The mixture was cooled to 0° C. and diluted with saturated aqueous sodium hydrogen carbonate solution. The phases were separated and the organic phase was dried over magnesium sulfate and concentrated under reduced pressure. The residue purified by column chromatography on silica gel, eluting with a mixture of ethyl acetate and dichloromethane (0:1 to 1:4 by volume) to afford the title compound as a white foam (0.20 g).

1. temperatureThe mixture was cooled to 0° C.
2. customThe phases were separated
3. dry with materialthe organic phase was dried over magnesium sulfate
4. concentrationconcentrated under reduced pressure
5. customThe residue purified by column chromatography on silica gel
6. washeluting with a mixture of ethyl acetate and dichloromethane (0:1 to 1:4 by volume)