Citric Acid → HCID 66816147, compound

Participants

Reaction Conditions

Reaction Steps

A 10% aqueous citric acid solution (0.14 ml, 0.067 mmol) was added to a solution of N-[2-(tert-butyl-dimethyl-silanyloxy)-ethyl]-N-(3-methyl-4-{(E)-2-[4-oxo-2-(3-trifluoromethoxy-phenyl)-1,3,8-triaza-spiro[4.5]dec-1-ene-8-sulfonyl]-vinyl}-phenyl)-methanesulfonamide (14.3 mg, 0.0192 mmol) in acetonitrile (0.2 ml), and the mixture was stirred at 60° C. for 2.5 hours. The reaction mixture was diluted with ethyl acetate, and the organic layer was washed with an aqueous sodium bicarbonate solution, dried over MgSO4 and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (ethyl acetate) to give N-(2-hydroxy-ethyl)-N-(3-methyl-4-{(E)-2-[4-oxo-2-(3-trifluoromethoxy-phenyl)-1,3,8-triaza-spiro[4.5]dec-1-ene-8-sulfonyl]-vinyl}-phenyl)-methanesulfonamide (12.5 mg, 100%).

Provenance & Evidence