Armstrong Teasdale LLP
Method for preparing apremilast
Provided is a method for preparing apremilast of formula I. Method one: (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine N-acetyl-L-leucine salt of formula II is reacted with 3-acetylaminophthalic anhydride of formula III in an aprotic solvent to produce the compound of formula I; method two: (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine N-acetyl-L-leucine salt of formula II is reacted with 3-acetylaminophthalic anhydride of formula III in an organic solvent in the presence of an organic alkali or an alkali metal hydride to produce the compound of formula I. The method for preparing apremilast requires inexpensive raw materials and reagents, is suitable for industrial production, and has great economic effects.
ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD
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C07C C07C C07D C07D C07C C07C
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Lianchao Jiegen Xiaoqiu
Zhou Liu Du