Reaktion #610763

Reaktionsgleichung

benzyl 3-oxo-2,4-diazabicyclo[3.1.0]hexane-2-carboxylate

4-bromo-2-methoxypyridine

xantphos

cesium carbonate

→

product

Ausbeute 41.1%

benzyl 4-(2-methoxypyridin-4-yl)-3-oxo-2,4-diazabicyclo[3.1.0]hexane-2-carboxylate

Ausbeute 41.1%

Lösungsmittel

1,4-dioxane

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigereagents and reaction conditions
2. 2
   SonstigePurification by column chromatography on silica gel (50% ethyl acetate in hexane)
3. 3
   Sonstigeafforded (35% ethyl acetate in hexane)

Vorschrift

Using analogous reagents and reaction conditions as described in Example 1 above, benzyl 3-oxo-2,4-diazabicyclo[3.1.0]hexane-2-carboxylate (50 mg, 0.215 mmol) was reacted with 4-bromo-2-methoxypyridine (44.5 mg, 0.237 mmol), xantphos (11 mg, 0.019 mmol), Pd2(dba)3 (6.0 mg, 0.006 mmol), cesium carbonate (105 mg, 0.32 mmol) and 1,4-dioxane (3.0 mL) in seal tube at 100° C. for 2.5 hours. Purification by column chromatography on silica gel (50% ethyl acetate in hexane) afforded (35% ethyl acetate in hexane) afforded 30 mg of the product (41% yield).

Quelle