2-Amino-4-methylpyridine → HCID 90067537, compound

Participants

Reaction Conditions

Reaction Steps

To a mixture of tert-butyl 4-(2-chloro-6-(2-hydroxyethyl(methyl)amino)-4-pyridyl)-5,6-dihydro-2H-pyridine-1-carboxylate (220 mg, 0.60 mmol), 4-methylpyridin-2-amine (71.13 mg, 0.66 mmol), sodium tert-butoxide (86.2 mg, 0.90 mmol), 2-dicyclohexylphosphino-2′,6′-diisopropoxybiphenyl (34.9 mg, 0.075 mmol), and RuPhos palladium(II) phenethylamine chloride (43.6 mg, 0.06 mmol) in 1,4-dioxane (3.0 mL) was capped in a small CEM microwave vial, de-gassed with N2, and heated in microwave at 120° C. for 15 min. It was concentrated onto Celite, purified by column chromatography (ISCO), 12 g column, eluded with 0-5% MeOH/DCM to give 135 mg (51%) of the title compound as a yellow gum. LC-MS: m/z=440 (M+H+).

Provenance & Evidence