反应详情

温度

45 °C

In a 25 mL round-bottomed flask, 1-(3-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-2-(hydroxymethyl)phenyl)-6-(2-(dimethylamino)ethylamino)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile (19 mg, 34.3 μmol, Eq: 1.00) and [hydrogen bis(dimethylphosphinito-kP)]platinum (II) (1.47 mg, 3.43 μmol, Eq: 0.1) were combined with Ethanol (271 μl) and Water (271 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, then 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-(2-dimethylamino-ethylamino)-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid amide (14.2 mg, 71%, [M+H]+ 572).

1. customto give a colorless solution
2. customThe crude reaction mixture
3. concentrationwas concentrated in vacuo
4. additiondiluted with acetonitrile and water
5. filtrationfiltered