Cesium carbonate → Ethyl 3-(4-cyano-1H-indazol-1-yl)-2,2-dimethylpropanoate

Beteiligte Stoffe

Reaktionsschritte

1H-Indazole-4-carbonitrile (commercially available from Insight Chemical Solutions Ltd.) (500 mg, 3.49 mmol), ethyl 3-bromo-2,2-dimethylpropanoate (D98) (803 mg, 3.84 mmol) and Cs2CO3 (1.36 g, 4.19 mmol) in dry DMF (3 ml) was heated to 80° C. overnight and then for a further 7 hours. The reaction mixture was then partitioned between EtOAc and H2O. The two layers were separated and the organic phase was washed with more H2O, brine, dried and concentrated a yellow oil. Purification of the residue by flash chromatography on silica gel [gradient ethyl acetate/cyclohexane] gave the title compound (356 mg, 37%) as a crystalline material. MS (ES) C15H17N3O2 requires 271, found 272 [M+H]+

Herkunft & Nachweise