Cesium carbonate → 8-Quinoxalin-2-yl-3,8-diaza-bicyclo[4.2.0]octane-3-carboxylic acid tert-butyl ester

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Reaction Conditions

Reaction Steps

To a mixture of 3,8-diaza-bicyclo[4.2.0]octane-3-carboxylic acid tert-butyl ester (Intermediate 1, 1.07 g, 5.05 mmol) and 2-chloro-quinoxaline (1.02 g, 6.06 mmol) in DMF (20.0 mL) was added Cs2CO3 (3.95 g, 12.1 mmol). The reaction mixture was heated at 80° C. for 16 h then cooled to ambient temperature. The reaction mixture was partitioned between water (400 mL) and ethyl acetate (50 mL) twice. The organic layers were combined and washed with water. The organic layers were dried (Na2SO4), filtered and concentrated under reduced pressure to yield crude title compound (1.84 g) which was used in the next step without purification.

Provenance & Evidence