1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 16222145, compound

Participants

Reaction Steps

1-{4-[(Ethylamino)carbonyl]phenyl}-5-(4-fluorobutyl)-1H-1,2,3-triazole-4-carboxylic acid (375 mg, 1.12 mmol) obtained in Example 108b), HOBt (76.5 mg, 0.561 mmol, 0.5 eq.) and cyclopropylamine (0.104 ml, 1.46 mmol, 1.3 eq.) were dissolved in acetonitrile-DMF (2:1, 4.5 ml), WSC (263 mg, 1.35 mmol, 1.2 eq.) was added, and the mixture was stirred at room temperature for 4 hr. The reaction mixture was diluted with 2% aqueous sodium carbonate solution (5 ml) and water (10 ml), and the mixture was stirred at room temperature. The precipitate was collected by filtration, washed with water and dried to give the title compound as a white powder (369 mg, 0.988 mmol, 88.2%).

Provenance & Evidence