5-Bromo-3-methyl-2-pyrazinamine

(iii) To a solution of a) 3-(N-(3-((5-amino-6-methylpyrazin-2-yl)ethynyl)-2, 4-difluorophenyl)sulfamoyl)-5-chloro-2-methoxybenzyl Acetate A mixture of 5-chloro-3-(N-(3-ethynyl-2, 4-difluorophenyl)sulfamoyl)-2-methoxybenzyl acetate (200 mg), dichlorobis(tricyclohexylphosphine)palladium(II) (34.3 mg), DIPEA (2 mL), copper(I) iodide (17.7 mg), Example 31 N-(3-((5-amino-6-methylpyrazin-2-yl)ethynyl)-2, 4-difluorophenyl)-5-chloro-2-methylbenzenesulfonamide A mixture of 5-chloro-N-(3-ethynyl-2, 4-difluorophenyl)-2-methylbenzenesulfonamide (100 mg), Example 110 N-(3-((5-amino-6-methylpyrazin-2-yl)ethynyl)-2, 4-difluorophenyl)-5-chloro-2-methoxypyridine-3-sulfonamide A mixture of 5-chloro-N-(3-ethynyl-2, 4-difluorophenyl)-2-methoxypyridine-3-sulfonamide (108 mg), A solution of 5-bromo-3-methyl-pyrazin-2-amine (1000 mg, 5.32 mmol), phenol (650 mg, 6.91 mmol), Cs2C03 (2600 mg, 7.98 mmol), Cul (203 mg, 1.06 mmol), and Nu, Nu-dimethylgly cine (110 mg, 1.06 mmol) in dioxane (5 mL) was degassed and heated to 90 C under N2 for 12 h. After cooling to room temperature, the mixture was diluted with EtOAc (100 mL) and water (100 mL) and the organic phase collected. The aqueous layer was extracted again with EtOAc (100 mL) and the combined organic layers were dried over anhydrous MgSC^ and concentrated to dryness. The residue was purified by flash column chromatography to give the title compound as a yellow oil (533 mg, 49.8% yield). MS (ESI): mass calcd. for CnHnN30, 201.1; m/z found, 202.1 [M+H]+.A solution of 5-bromo-3-methyl-pyrazin-2-amine (1000 mg, 5.32 mmol), phenol (650 mg, 6.91 mmol), Cs 2CO 3 (2600 mg, 7.98 mmol), CuI (203 mg, 1.06 mmol), and N, N-dimethylglycine (110 mg, 1.06 mmol) in dioxane (5 mL) was degassed and heated to 90 under N 2 for 12 h. After cooling to room temperature, the mixture was diluted with EtOAc (100 mL) and water (100 mL) and the organic phase collected. The aqueous layer was extracted again with EtOAc (100 mL) and the combined organic layers were dried over anhydrous MgSO 4 and concentrated to dryness. The residue was purified by flash column chromatography to give the title compound as a yellow oil (533 mg, 49.8% yield). MS (ESI) : mass calcd. for C11H 11N 3O, 201.1 m/z found, 202.1 [M+H] +.A mixture of

Molecular Weight:188.03
XLogP3:0.9
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Exact Mass:186.97451
Monoisotopic Mass:186.97451
Topological Polar Surface Area:51.8
Heavy Atom Count:9
Complexity:98.2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes