反应详情

To a solution of 0.91 g (2.8 mmol) [2-phenyl-5-(4-propyl-cyclohexyl)-pyrrol-1-yl]-acetic acid in 28 mL anhydrous DMF was added 2.27 g (14 mmol) carbonyldiimidazole. The reaction was stirred at room temperature for 50 min, upon which time was added 2.52 g (14 mmol) guanidine carbonate, 0.17 g (1.4 mmol) 4-dimethylaminopyridine, and 2.83 g (28 mmol) triethylamine. The reaction was stirred at room temperature over 16 hr. The solution was filtered to remove the precipitate that formed, was diluted with ethyl acetate, and was washed three times with brine. Drying over MgSO4 and concentration afforded 1.49 g of N-{2-[2-phenyl-5-(4-propyl-cyclohexyl)-pyrrol-1-yl]-acetyl}-guanidine as a yellow-brown oil. The product was observed to contain DMF by 1H NMR. However, it was used in the next step without further purification.

1. stirringThe reaction was stirred at room temperature over 16 hr
2. filtrationThe solution was filtered
3. customto remove the precipitate
4. customthat formed
5. washwas washed three times with brine
6. dry with materialDrying over MgSO4 and concentration