扎托洛芬的合成

Synthesis of Zaltoprofen

2-(3-羧甲基-4-苯硫基苯基)丙酸与甲醇酯化生成2-(3-甲氧羰基甲基-4-苯硫基苯基)丙酸甲酯,然后与多聚磷酸环合,水解制得扎托洛芬,总收率89%,纯度99.3%。该工艺操作简便,收率高,易于工业化生产。

Zaltoprofen was synthesized from 2-（3-carboxymethyl-4-phenylthiophenyl）propionic acid via esterification with methanol to give methyl 2-（3-methoxycarboxymethyl-4-phenylthiophenyl）propionate, which was subjected to cyclization with polyphosphoric acid, and hydrolysis with an overall yield of 89% and a purity of 99.3 %. This process was suitable for industrial production with simple operation and high yield.