Hydrochloric Acid → HCID 59331622, compound

Participants

Reaction Steps

To a solution of 2-{1-[4-(cyclopropylsulfonyl)phenyl]-2-(tetrahydro-2H-pyran-4-yl)ethyl}-5-(1,3-thiazol-2-yl)-1H-pyrrole-3-carboxylic acid (0.066 g) in N,N-dimethylformamide (5 mL) were added N,N-dimethylamine (0.038 mL), 0-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (57 mg) and N,N-diisopropylethylamine (0.069 mL), and the mixture was stirred at room temperature for 16 hr. To the reaction mixture was added 1M hydrochloric acid, and the mixture was extracted with ethyl acetate. The extract was washed successively with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate:hexane=70:30-100:0, volume ratio), and recrystallized from hexane-ethyl acetate to give the title compound (0.058 g, yield 84%) as colorless crystals. MS: 514 (MH+). melting point 180-182° C.

Provenance & Evidence