Reaktion #1462595

Reaktionsgleichung

5-amino-4-(methylamino)-2-[[4-(morpholin-4-yl)phenyl]amino]pyrimidine

ethyl 2-(3,5-dibromopyridin-4-yl)-2-oxoacetate

HOAc

→

title compound

Ausbeute 26.2%

6-(3,5-Dibromopyridin-4-yl)-8-methyl-2-[[4-(morpholin-4-yl)phenyl]amino]-8H-pteridin-7-one

Ausbeute 26.2%

Lösungsmittel

2-methoxyethanol

EtOAc

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturis heated
2. 2
   Temperaturunder reflux for 18 hours
3. 3
   Wascheneluting with CH2Cl2/EtOAc (4:1)

Vorschrift

A mixture of 0–30 g (1 mmol) of 5-amino-4-(methylamino)-2-[[4-(morpholin-4-yl)phenyl]amino]pyrimidine, 0.67 g (2 mmol) of ethyl 2-(3,5-dibromopyridin-4-yl)-2-oxoacetate (from preparation 17), and 0.5 mL of HOAc in 15 mL of 2-methoxyethanol is heated under reflux for 18 hours. Workup in EtOAc, followed by chromatography on silica, eluting with CH2Cl2/EtOAc (4:1), gives 0.15 g (26%) of the title compound (Compound 19): mp (EtOH) 204–206° C.

Quelle