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HRID 16456Erstellt: 23. Oktober 2026

Dimethylformamide → N4-[3-Fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-6-morpholin-4-yl-pyrimidine-2,4-diamine

https://huagongshe.com/de/reaction/16456

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktDimethylformamideHCID 6228—
EduktMorpholineHCID 8083—
EduktDiisopropylethylamineHCID 81531—
Edukt6-Chloro-N4-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]pyrimidine-2,4-diamineHCID 58733241—
Lösungsmittel2-EthylhexanolHCID 7720—
ProduktN4-[3-Fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-6-morpholin-4-yl-pyrimidine-2,4-diamineHCID 58733326—

Reaktionsbedingungen

Temperatur150 °C

Reaktionsschritte

52 mg (0.14 mmol) of 6-chloro-N4-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-phenyl]pyrimidine-2,4-diamine (from example 60) are dissolved in 2.5 ml of 2-ethylhexanol. 0.24 ml of N-ethyldiisopropylamine and 36 mg (0.42 mmol) of morpholine are added, and the mixture is heated at 150° C. bath temperature for 20 hours. After cooling, a little DMF is added and the mixture is chromatographed on silica gel 60 (gradient column: mobile phase: DCM:methanol=50:1, then 3:1). This gives an oil which is purified by preparative HPLC.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS07737153B2
Quelldatensatzuspto-grants-2010_06
ORD IDord-f27cdbac85644e37bba24b36a57db768
Quellennotizuspto-grants-2010_06