Synthetic method of medicine apremilast for treating psoriasis arthritis disease

The invention discloses a synthetic method of medicine apremilast for treating a psoriasis arthritis disease. The method includes the steps: taking 3-ethoxy-4-methoxybenzaldehyde as a starting material; reacting the starting material with dimethyl sulfone and n-butyllithium to obtain 3-ethoxy-4-meth...

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Bibliographische Detailangaben
Hauptverfasser: ZHANG JINGXIA, ZHANG LIANTAO
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthetic method of medicine apremilast for treating a psoriasis arthritis disease. The method includes the steps: taking 3-ethoxy-4-methoxybenzaldehyde as a starting material; reacting the starting material with dimethyl sulfone and n-butyllithium to obtain 3-ethoxy-4-methoxyl-alpha-[(methylsulfonyl) methyl]-benzyl alcohol; performing oxidation reaction to obtain 1-(3-ethoxy-4-methoxybenzaldehyde phenyl)-2-methylsulfonyl-aceton; performing reduction reaction to obtain R-3-ethoxy-4-methoxyl-alpha-[(methylsulfonyl) methyl]-phenylcarbinol; performing Mitsunobu reactionon the R-3-ethoxy-4-methoxyl-alpha-[(methylsulfonyl) methyl]-phenylcarbinol and 3-acetamido-phthalimide to obtain a target product apremilast. The synthetic method has the advantages of mild reactioncondition, simple process, good yield, easiness in industrialization and the like. 本发明公开了种治疗银屑病性关节炎疾病的药物阿普斯特的合成方法,该方法以3-乙氧基-4-甲氧基苯甲醛为起始原料,经与二甲基砜、正丁基锂的反应,得到3-乙氧基-4-甲氧基-α-[(甲磺酰基)甲基]-苯甲醇,通过氧化反应获得1-(3-乙氧基-4-甲氧基苯基)-2-甲磺酰基-乙酮,再通过还原反