Reaktion #610765

Reaktionsgleichung

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

4-bromo-2-(trifluoromethyl)pyridine

xantphos

cesium carbonate

→

product

Ausbeute 74.0%

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

Ausbeute 74.0%

Lösungsmittel

1,4-dioxane

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigereagents and reaction conditions
2. 2
   Sonstigeto yield the crude product
3. 3
   SonstigePurification by column chromatography on silica gel (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 (100 mg, 0.43 mmol) was heated with 4-bromo-2-(trifluoromethyl)pyridine (107 mg, 0.474 mmol), xantphos (22.36 mg, 0.038 mmol), Pd2(dba)3 (12 mg, 0.012 mmol), cesium carbonate (210 mg, 0.64 mmol) and 1,4-dioxane (6.0 mL) at 100° C. for 1 hour to yield the crude product. Purification by column chromatography on silica gel (35% ethyl acetate in hexane) afforded 120 mg of the product (74% yield).

Quelle