Cesium fluoride → HCID 70978278, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 1,5-dichloro-3-(2-methoxyethoxy)isoquinoline (578 mg, 2.124 mmol) in DMSO (5 mL) was added CsF (323 mg, 2.124 mmol) and heated to 140° C. for 2 hrs. LC/MS showed the desired product. The reaction was diluted with ethyl acteate and washed with water, and brine. The organic phase was collected, dried over MgSO4, and concentrated under vacuum to give the crude product as a reddish brown solid. Crude product purified via biotage (90 g column, 5-50% EtAOc:Hex) to give the product 5-chloro-1-fluoro-3-(2-methoxyethoxy)isoquinoline (250 mg, 46% yield) as a light yellow solid. MS: MS m/z 256.15(M++1).

Provenance & Evidence