1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 57664878, compound

Participants

Reaction Steps

1-{4-[(Ethylamino)carbonyl]phenyl}-5-(5-fluoropentyl)-1H-1,2,3-triazole-4-carboxylic acid (353 mg, 1.01 mmol) obtained in Example 111b), HOBt (55.3 mg, 0.405 mmol, 0.4 eq.) and cyclopropylamine (0.094 ml, 1.32 mmol, 1.3 eq.) were dissolved in acetonitrile-DMF (2:1, 4.5 ml), WSC (218 mg, 1.11 mmol, 1.1 eq.) was added, and the mixture was stirred at room temperature for 12.5 hr. The reaction mixture was diluted with 2% aqueous sodium carbonate solution (20 ml), and the mixture was stirred at room temperature. The precipitate was collected by filtration, washed with water and dried to give a white powder. This was crystallized from ethyl acetate-diethyl ether, and the precipitate was collected by filtration, washed with diethyl ether and dried to give the title compound as a white powder (333 mg, 0.859 mmol, 85.1%).

Provenance & Evidence