Reaktion #1112808

Reaktionsgleichung

1-(3-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-2-(hydroxymethyl)phenyl)-6-morpholino-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile

ethanol

→

1-[3-(6-tert-Butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-6-morpholin-4-yl-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid amide

Ausbeute 90.0%

Lösungsmittel

water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigeto give a colorless solution
2. 2
   Einengenconcentrated in vacuo
3. 3
   workup.ADDITIONMixture was diluted with acetonitrile and water
4. 4
   Filtrationfiltered

Vorschrift

In a 25 mL round-bottomed flask, 1-(3-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-2-(hydroxymethyl)phenyl)-6-morpholino-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile (75 mg, 136 μmol, Eq: 1.00) and [hydrogen bis(dimethylphosphinito-kP)]platinum (II) (2 mg, 4.66 μmol, Eq: 0.0343) were combined with ethanol (1 ml) and water (1.00 ml) to give a colorless solution. The reaction mixture was heated to 45° C. and stirred for 1 h, then 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-morpholin-4-yl-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid amide (70 mg, 90%, [M+H]+ 571).

Quelle