Imidazole → HCID 68841301, compound

Participants

Reaction Steps

90 mg of imidazole and 250 μl of diphenylphosphinyl chloride are added to a solution of 140 mg of 3-(1-tert-butoxycarbonyl-2,3-dihydro-1H-indol-2-yl)-5-hydroxyindazole-1-carboxylic acid tert-butyl ester in 15 ml of dichloromethane. The reaction medium is stirred at ambient temperature overnight. After dilution with 10 ml of dichloromethane and 10 ml of distilled water, the medium is separated by settling out. The organic phase is dried over magnesium sulfate, filtered, and concentrated under reduced pressure in a rotary evaporator. The crude is taken up in a dichloromethane/methanol mixture and the solid is filtered off. After concentration under reduced pressure, the filtrate is purified by flash chromatography, eluent: cyclohexane/ethyl acetate 8:2 to obtain 200 mg of 3-(1-tert-butoxycarbonyl-2,3-dihydro-1H-indol-2-yl)-5-(diphenylphosphinoyloxy)indazole-1-carboxylic acid tert-butyl ester.

Provenance & Evidence