Using pyridine as the catalyst and sulfoxide chloride as the chlorinated reagent,acetylsalicylic acid underwent substitution reaction to give acetylsalicyloyl chloride.Then,using tetrahydrofuran as the solvent to dissolve the acetylsalicyloyl chloride and TBAB as the phase transfer catalyst,acetaminophen was condensed with acetylsalicyloyl chloride for 60 minutes to give benorilate under the alkaline condition of 5％sodium hydroxide.The mole ratio of acetaminophen to acetylsalicylic acid is 1∶1.2.The synthesis process is mild,with simple post-treatment and purification.The total yield is 69％.The target product was structurally confirmed by 1H-NMR and 13C-NMR.
benorilatesynthesisoptimizationphase transfer catalyst
NETL
NSTL
万方数据
