t-Butylammonium fluoride → 4-(4-{2-[(2r)-2-Hydroxy-2-(4-hydroxy-3-methanesulfonylamino-phenyl)-ethylamino]-ethyl}-phenylamino)-piperidine-1-carboxylic acidoctylamide

Participants

Reaction Steps

4-{4-[2-({(2R)-2-{4-(Benzyloxy)-3-[(methylsulfonyl)amino]phenyl}-2-[(triethylsilyl)oxy]ethyl}amino)ethyl]anilino}-N-octyl-1-piperidinecarboxamide was dissolved in anhydrous tetrahydrofuran and tert-butylammonium fluoride (1 M in tetrahydrofuran) added. The reaction was stirred at ambient temperature for 4 days. The solvent was removed in vacuo and the residue purified by flash chromatography on silica gel Merck-60 (eluant: 20:1 going to 10:1 chloroform-methanol containing 2% triethylamine) to furnish the title compound (0.36 g, 0.519 mmol).

Provenance & Evidence