反应详情

温度

100 °C

To a mixture of (3S)-1-(2-chloropyrimidin-4-yl)-3-isopropyl-2-oxopyrrolidine-3-carbonitrile (200 mg) obtained in Step A of Example 9, tert-butyl 3-(4-amino-1H-pyrazol-1-yl)azetidine-1-carboxylate (97 mg) obtained in Step B of Example 131, cesium carbonate (370 mg) and dicyclohexyl(2′,4′,6′-triisopopropyl-3,6-dimethoxybiphenyl-2-yl)phosphine (57 mg) in tert-butanol (2.0 mL) was added tris(dibenzylideneacetone)dipalladium(0) (48 mg), and the mixture was stirred at 100° C. for 5 hr. The insoluble substance was removed by filtration through Celite, 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 (22 mg).

1. customThe insoluble substance was removed by filtration through Celite
2. customthe solvent was evaporated under reduced pressure
3. customThe residue was purified by silica gel column chromatography (hexane/ethyl acetate)