【药物名称】
化学结构式(Chemical Structure):
参考文献No.656643
标题:Design and synthesis of a novel L-dopa-entacapone codrug
作者:Lepp鋘en, J.; Huuskonen, J.; Nevalainen, T.; Gynther, J.; Taipale, H.; Jarvinen, T.
来源:J Med Chem 2002,45(6),1379
合成路线图解说明:

Esterification of L-Dopa (I) with thionyl chloride in methanol leads to the methyl ester (II). The phenolic hydroxyls of (II) are further acylated by acetyl chloride in trifluoroacetic acid to produce diacetate (III). Treatment of the protected derivative of L-Dopa (III) with diphosgene gives rise to isocyanate (IV). This is then coupled to entacapone (V) in refluxing acetonitrile to furnish carbamate (VI). The acetate ester groups of (VI) are finally removed by treatment with 3N HCl in acetone.

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