Synthesis Of Benzoylformic Acid And Its Methyl Ester

Benzoylformic acid and its methyl ester, which show various special chemical behaviors because of their multiple reaction centers in structures, are important pharmaceutical intermediates used for the preparation of some drugs and many functional materials to promote physiological metabolic balance and to enhance anti-aging function.A novel process for the synthesis of benzoylformic acid and its methyl ester was studied using a-bromoacetophenone based on styrene as precursor through oxidation, carbonyl-protection, hydrolysis, deprotection and oxidation reactions. Followed by the esterification with anhydrous methanol, the methyl benzoylformate was conveniently prepared in the presence of TiO2/SO42-catalyst with cyclohexane as water-carrying agent. The reaction mechanisms and influencing factors on reactions were discussed in details. a-Bromoacetophenone could be selectively synthesized by one-pot process under optimal conditions.The products structures were characterized by HPLC, IR,1H-NMR and GC-MS.