abstract |
The present invention relates to a synthetic method of dronedarone. The method comprises the following steps: Step 1, the preparation of 2-chloromethyl-4-nitrophenol: taking p-nitrophenol as raw material, adding concentrated hydrochloric acid or phosphoric acid Under catalysis, condense with paraformaldehyde and concentrated hydrochloric acid to obtain 2-chloromethyl-4-nitrophenol, the preparation of step 2, 2-hydroxyl-5-nitrobenzyltriphenylphosphonium chloride: 2-chloromethyl Base-4-nitrophenol and triphenylphosphine reflux reaction in chloroform, step 3, preparation of 2-n-butyl 5-nitrobenzofuran: 2-hydroxy-5-nitrobenzyl triphenyl chloride Phosphonium chloride is condensed with n-valeryl chloride in toluene solution under the catalysis of triethylamine and n-valeric acid to obtain 2-n-butyl 5-nitrobenzofuran. |