Morpholine → HCID 117840499, compound

Participants

Reaction Steps

To a solution of 2-(4-((4-((3S)-3-cyano-3-cyclopropyl-2-oxopyrrolidin-1-yl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)-2-methylpropanoic acid hydrochloride (80 mg) obtained in Example 108 in N,N-dimethylformamide (2.0 mL) were added 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (58 mg), 1-hydroxybenzotriazole monohydrate (57 mg), N,N-diisopropylethylamine (97 μL) and morpholine (19 mg), and the mixture was stirred overnight at room temperature. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (NH, hexane/ethyl acetate). To a solution of the residue (87 mg) in ethanol (3.0 mL) was added dropwise 1 M hydrochloric acid (0.19 mL), the mixture was stirred for 5 min, and the solvent was evaporated under reduced pressure. The residue was recrystallized (ethanol/diisopropyl ether) to give the title compound (35 mg).

Provenance & Evidence