| 摘要 |
PURPOSE: A preparation method of erdosteine is provided, thereby inhibiting oxidation of thioglycolic acid into dithiodiglycolic acid, and improving the preparation yield of erdosteine without an additional purification process. CONSTITUTION: The preparation method of erdosteine of the formula(I) comprises the steps of: reacting thioglycolic acid of the formula(II) with chloroacetic acid of the formula(III) to prepare thiodiglycolic acid of the formula(IV) in an organic solvent and an organic base in the presence of a catalyst; and reacting the thiodiglycolic acid of the formula (IV) with DL-homocysteine thiolactone hydrochloride of the formula(V), wherein the organic solvent is selected from acetone, acetonitrile, chloroform, dichloromethane, ethylacetate, methanol, ethanol and isopropanol; the organic base is selected from triethylamine, trimethylamine and pyridine; and the catalyst is dimethylformamide, dimethylacetamide, thionylchloride, and phosphorousoxychloride.
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