Potassium Phosphate, Tribasic → HCID 86703768, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of methyl 4-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethyl)-2-fluoro-5-iodobenzoate (70 mg, 0.12 mmol), cyclopropylboronic acid (16 mg, 0.18 mmol), potassium phosphate (102 mg, 0.48 mmol) and tricyclohexylphosphine tetrafluoroborate (9 mg, 0.024 mmol) in toluene (2 mL) and water (0.1 mL) under a nitrogen atmosphere was added palladium acetate (8 mg, 0.037 mmol). The reaction mixture was heated to 100° C. for 18 hours then cooled to ambient temperature. The reaction mixture was quenched with water (10 mL), extracted with ethyl acetate (10 mL×3). The combined organic layers were washed with brine (10 mL), dried over anhydrous sodium sulfate, filtered and concentrated to afford the target compound (70 mg, crude) which was used in the next step without purification. LCMS (ESI): m/z: 486.9 [M+H]+.

Provenance & Evidence