J. Shan, Fang Weizheng, Feng Bai-nian
2015
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Guangzhou Chemical Industry
Abstract
1-( 3-ethoxy-4-methoxyphenyl )-2-( methylsulfonyl ) ethanamine was pre- pared by 3-ethoxy-4-methoxybenzonitrile, the S-isomer compound was achieved by treatment of 3 with N-acetyl-L-leucine, then apremilast was prepared by condensation of 3-N-acetylaminophthalic anhydride with ( s ) 1-( 3-ethoxy-4-methoxyphenyl )-2-( methylsulfonyl) ethanamine. Compared to traditional synthetic methods, the total yield of the synthesis increased 30%. Apremilast, as an inhibitor of phosphodiesterase 4 ( PDE-4 ) , is an oral medication that inhibits the activity of multiple inflammatory markers involved in the pathogenesis of psoriasis. Therefore, a theoretical basis for further industrial production was provided.