Reaktion #1600829

Reaktionsgleichung

DEAD

4-(2-hydroxyethyl)morpholine

triphenylphosphine

2-fluoro-4-(3-((7-methoxyquinolin-4-yloxy)methyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)phenol

→

4-((6-(3-fluoro-4-(2-morpholinoethoxy)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)-7-methoxyquinoline

Lösungsmittel

THF

Reaktionsbedingungen

Aufarbeitung

1. 1
   EinengenConcentrated
2. 2
   SonstigePurified on RPHPLC
3. 3
   workup.ADDITIONFractions containing product
4. 4
   workup.ADDITIONwere treated with 9% sodium carbonate
5. 5
   Sonstigewas isolated by filtration

Vorschrift

To a mixture of 4-(2-hydroxyethyl)morpholine (0.0964 ml, 0.788 mmol), triphenylphosphine (0.238 g, 0.909 mmol), 2-fluoro-4-(3-((7-methoxyquinolin-4-yloxy)methyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)phenol (0.253 g, 0.606 mmol)(prepared according to General Method A) in THF (10 mL) was added DEAD (0.144 ml, 0.909 mmol). Stirred at room temperature for 1 h. Concentrated. Purified on RPHPLC. Fractions containing product were treated with 9% sodium carbonate. Removed volatiles in vacuo. Product crashed out and was isolated by filtration. MS m/z=531.2 [M+1]+. Calc'd for C28H27FN6O4: 530.5.

Quelle