Reaktion #1462593

Reaktionsgleichung

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

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

HOAc

→

title compound

Ausbeute 18.0%

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

Ausbeute 18.0%

Lösungsmittel

2-methoxyethanol

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturas heated
2. 2
   Temperaturunder reflux for 16 hours
3. 3
   WaschenChromatography on alumina, eluting 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, 0.37 g (1.5 mmol) of ethyl 2-(3,5-dichloropyridin-4-yl)-2-oxoacetate, and 0.3 mL HOAc in 15 mL 2-methoxyethanol as heated under reflux for 16 hours, and worked up as above in 2. Chromatography on alumina, eluting with CH2Cl2/EtOAc (4:1), gives 85 mg (18%) of the title compound (Compound 12 in Tables 1 and 2): mp (MeOH) 243–245° C.

Quelle