(1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)-1-(quinolin-3-yl)propan-2-amine bis(2,2,2-trifluoroacetate) (42a, 65 mg, 0.10 mmol) was dissolved in THF (1.5 mL), triethylamine (75 μl, 0.54 mmol) was added followed by cyclopropanesulfonyl chloride (15 μl, 0.15 mmol). The reaction mixture was stirred at room temperature, after 1.5 hours another portion of triethylamine (75 μl, 0.54 mmol) and excess of cyclopropanesulfonyl chloride (50 μl, 0.49 mmol) was added. The reaction mixture was left over night at room temperature. Solvent was removed by evaporation and the residual material was purified by HPLC. Yield 18 mg (34%).
