5-(phenylmethoxy)-1H-indole-2-carboxylic acid → HCID 66792775, compound

Participants

Reaction Steps

A mixture of 1-(2-tert-butylphenyl)piperazine dihydrochloride obtained in Reference Example 1 (2.0 g), 5-(benzyloxy)-1H-indole-2-carboxylic acid (2.03 g), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (1.92 g), 1-hydroxy-1H-benzotriazole monohydrate (1.53 g), triethylamine (2.79 mL), and N,N-dimethylformamide (30 mL) was stirred at room temperature for over-night. Water was added to the reaction solution, and the mixture was extracted with ethyl acetate. The ethyl acetate layer was washed with saturated brine, and dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure to provide the title compound (2.6 g, 81%) as crystals.

Provenance & Evidence