Imidazole → HCID 59370758, compound

Participants

Reaction Steps

(R)-Tert-butyl 6-(2-((2-(3-amino-4-fluorophenyl)-2-hydroxyethyl)(tert-butoxycarbonyl)amino)ethoxy)-3-chloroindazole-1-carboxylate (601.2 mg) which can be prepared according to the method described in Reference example 69, etc. and imidazole (290.3 mg; Tokyo Chemical Industry Co., Ltd) were dissolved in dehydrated DMF (5 mL), added with chlorotriethylsilane (705 μL; manufactured by Shin-Etsu Chemical Co., Ltd.), and then the mixture was stirred for three hours at room temperature. The reaction solution was added to saturated solution of sodium hydrogen carbonate solution and extracted twice with ethyl acetate. The organic layer was washed twice with water and once with brine, dried over anhydrous sodium sulfate, and then the solvent was evaporated under reduced pressure. The resulting residue was purified by column chromatography (“COLUMN-B”; n-hexane:ethyl acetate=84:16→64:36) to obtain the title compound (480 mg).

Provenance & Evidence