1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 178472213, compound

Participants

Reaction Steps

To a dichloromethane (10 mL) suspension of trans-6-[3-(2-fluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester (939 mg) obtained in Example 2, Meldrum's acid (317 mg), dimethylaminopyridine (293 mg), and EDCI (460 mg) were added at 0° C. The reaction mixture was diluted with dichloromethane, washed with 1 N hydrochloric acid and saturated brine, then dried over sodium sulfate, and then concentrated. A mixture of the residue and ethanol (10 mL) was heated to reflux for 4 hours and concentrated. The residue was purified by column chromatography (dichloromethane/ethyl acetate) to obtain the title compound (820 mg, 76%) as a yellowish-white solid.

Provenance & Evidence