1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 117840745, compound

Participants

Reaction Steps

To a solution of 4-((4-((3R)-3-cyano-3-ethyl-2-oxopyrrolidin-1-yl)pyrimidin-2-yl)amino)benzoic acid (100 mg) obtained in Example 231 in N,N-dimethylformamide (2.0 mL) were added 1-aminocyclopropanecarbonitrile hydrochloride (31 mg), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (46 mg), 1-hydroxybenzotriazole (40 mg) and triethylamine (56 μL), and the mixture was stirred overnight at room temperature. To the reaction mixture was added saturated aqueous sodium hydrogen carbonate solution, and the mixture was extracted with ethyl acetate. The obtained organic layer was washed with saturated brine, and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ethyl acetate) to give the title compound (38 mg).

Provenance & Evidence