Potassium Phosphate, Tribasic → HCID 86703773, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl 4-(1-benzhydrylazetidin-3-yloxy)-5-chloro-2-fluorobenzoate (700 mg, 1.50 mmol), cyclopropylboronic acid (258 mg, 3.00 mmol), tricyclohexylphosphine tetrafluoroborate (57 mg, 0.15 mmol), potassium phosphate (954 mg, 4.5 mmol) and palladium acetate (224 mg, 0.15 mmol) in toluene (20 mL) and H2O (1 mL) was stirred at 100° C. for 18 h. The mixture was filtered and diluted with ethyl acetate, washed with brine and concentrated. The residue was purified by silica gel chromatography (eluting with ethyl acetate/ petroleum ether from 0/10 to 1/10) to give target product (650 mg, 92%) as a yellow oil. LCMS (ESI) m/z: 474.2 [M+H].

Provenance & Evidence