Ethanol → 1-[3-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-6-(6-ethoxy-pyridin-3-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid amide

Participants

Reaction Conditions

Reaction Steps

In a 25 mL round-bottomed flask, 1-(3-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-2-(hydroxymethyl)phenyl)-6-(6-ethoxypyridin-3-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile (36 mg, 61.2 μmol) and [hydrogen bis(dimethylphosphinito-kP)]platinum (II) (263 μg, 0.612 μmol, Eq: 0.01) were combined with ethanol (480 μl) and water (480 μl) to give a colorless solution. The reaction mixture was heated to 45° C. and stirred for 1 h. The crude reaction mixture was concentrated in vacuo. Mixture was diluted with acetonitrile and water and filtered. The resultant filtrate was lyophilized to give 1-[3-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-6-(6-ethoxy-pyridin-3-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid amide (31 mg, 84%, [M+H]+ 607).

Provenance & Evidence