1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 178513917, compound

Participants

Reaction Steps

A DMF (15 mL) solution of trans-6-[3-(2-fluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester (527 mg) obtained in Example 2, HOBt (166 mg), EDCI (236 mg), and ammonia water (0.5 mL) was stirred at room temperature for 2 days. The reaction mixture was diluted with ethyl acetate, washed with a saturated aqueous solution of sodium bicarbonate and saturated brine, then dried, and concentrated. The residue was purified by chromatography (NH silica gel, dichloromethane/methanol=30:1→5:1) to obtain a solid. This solid was recrystallized (isopropanol) to obtain the title compound (89 mg, 17%) as a white solid.

Provenance & Evidence