4-(2-Cyanoprop-2-yl)benzeneboronic acid → 2-{4-[5-Amino-6-(1-oxo-1,2,3,4-tetrahydro-isoquinolin-6-yl)-pyrazin-2-yl]-phenyl}-2-methyl-propionitrile

Participants

Reaction Steps

General method B was applied to 4-(2-cyanopropan-2-yl)phenylboronic acid (79 mg, 0.42 mmol) and 6-(3-amino-6-bromopyrazin-2-yl)-3,4-dihydroisoquinolin-1(2H)-one (150 mg, 0.38 mmol) in n-butanol (2 mL) to give 2-{4-[5-amino-6-(1-oxo-1,2,3,4-tetrahydro-isoquinolin-6-yl)-pyrazin-2-yl]-phenyl}-2-methyl-propionitrile (119 mg, 82% yield) after purification by column chromatography on silica (2-5% MeOH/DCM eluent).

Provenance & Evidence