Sulbutamol was synthesized from 5-bromosalicylaldehyde via reduction, benzyl protection, Suzuki-Miyaura coupling reaction, addition of double bond, nucleophilic substitution, Pd/C reduction. The total yield was 56.0% (based on 5-bromosalicylaldehyde). The optimistic condition of Suzuki-Miyaura coupling reaction was established. The optimum reaction conditions were obtained as follows: n(intermediate II) : n(potassium vinyltrifluoroaborate) : n(palladium chloride) : n(triphenylphosphine) : n(cesium carbonate) = 1:1.2:0.02:0.06:2. The reaction was refluxed in tetrahydrofuran / water (volume ratio 9:1, 0.5 mol / L, based on the amount of intermediate II substance) mixed solvent for 12 hours. The structure of salbutamol and the important intermediates were confirmed by HRMS, 1H NMR and 13C NMR. The synthetic route here is suitable for the amplification and preparation of salbutamol and has the value of industrial application because of the mild reaction condition, easy control as well as simple equipment and operation without purification by column chromatography.