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With hydrazine In 1,4-dioxane at 150℃; for 0.5 h; Microwave irradiation; Sealed tube
Example 86.2-(6,7-Difluoro-l-methyl-lH-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid [(R)-2- (3-cyano-azetidin-l -yl)-l -methyl-2-oxo-ethyl]-amideIn a microwave vial 2,3,4-trifluorobenzaldehyde (1.5 g, 9.4 mmol) was dissolved in 1 ,4-dioxane(6 mL) and hydrazine (6 mL, 191 mmol) was added. The vial was sealed and heated under microwave irradiation at 150°C for 30 min. The reaction was quenched with water and extracted with EtOAc. The organic layer was washed with brine then dried over MgSC^ and concentrated. The residue was purified by silica gel chromatography with 20percent to 50percent EtO Ac/heptane to provide 664 mg (46percent>) of 6,7-difluoro-lH-indazole as a light brown powder. 1H NMR (CDCI3, 300 MHz): ? (ppm) 8.10 (d, J=3.4 Hz, IH), 7.47 (dd, J=8.9, 4.0 Hz, IH), 7.05 (ddd, J=10.6, 8.9, 6.6 Hz, IH).
With hydrazine; In 1,4-dioxane; at 150℃; for 0.5h;Microwave irradiation; Sealed tube;
Example 86.2-(6,7-Difluoro-l-methyl-lH-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid [(R)-2- (3-cyano-azetidin-l -yl)-l -methyl-2-oxo-ethyl]-amideIn a microwave vial <strong>[161793-17-5]2,3,4-trifluorobenzaldehyde</strong> (1.5 g, 9.4 mmol) was dissolved in 1 ,4-dioxane(6 mL) and hydrazine (6 mL, 191 mmol) was added. The vial was sealed and heated under microwave irradiation at 150C for 30 min. The reaction was quenched with water and extracted with EtOAc. The organic layer was washed with brine then dried over MgSC^ and concentrated. The residue was purified by silica gel chromatography with 20% to 50% EtO Ac/heptane to provide 664 mg (46%>) of 6,7-difluoro-lH-indazole as a light brown powder. 1H NMR (CDCI3, 300 MHz): ? (ppm) 8.10 (d, J=3.4 Hz, IH), 7.47 (dd, J=8.9, 4.0 Hz, IH), 7.05 (ddd, J=10.6, 8.9, 6.6 Hz, IH).
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