Cesium carbonate → Benzyl 3-oxo-4-(2-(trifluoromethyl)pyridin-4-yl)-2,4-diazabicyclo[3.1.0]hexane-2-carboxylate

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Reaction Steps

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).

Provenance & Evidence