Triethylamine → HCID 117840780, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 3-cyclopropyl-3-(hydroxymethyl)-1-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)pyrrolidin-2-one (45 mg) obtained in Example 393 in tetrahydrofuran (1.0 mL) were added methanesulfonyl chloride (15 μL) and triethylamine (29 μL) at 0° C., and the mixture was stirred at 0° C. for 1 hr. 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. To a solution of the residue in N,N-dimethylformamide (1.0 mL) were added potassium cyanide (36 mg) and sodium iodide (82 mg) at room temperature, and the mixture was stirred overnight at 120° C. 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 (17 mg).

Provenance & Evidence