Hydrochloric Acid → HCID 131730801, compound

Participants

Reaction Steps

3-[1-(3-Trifluoromethyl-benzenesulfonyl)-1H-indol-5-yl]-azetidine-1-carboxylic acid tert-butyl ester (compound 13) (400 mg, 0.83 mmol) was dissolved in formic acid (4.7 ml) at 0° C. and stirred for 2 hours. The reaction mixture was evaporated to dryness at 30° C. The residue was dissolved in ethyl acetate (50 ml), and washed with a 1 molar aqueous solution of NaOH (10 ml). The organic layer was dried over magnesium sulphate, filtered, and evaporated to dryness to yield the crude product (231 mg, 82%). The crude product was dissolved in ether (50 ml), treated with a solution of hydrochloric acid in ether, and the precipitate was collected to give the product (151 mg, 44%).

Provenance & Evidence