CAJ | 학술논문

以3-乙氧基-4-甲氧基苯腈为原料制备得到1-(3-乙氧基-4-甲氧基-苯基)-2-甲磺酰基-乙酮，然后通过N-乙酰基L-亮氨酸经化学拆分得到S型异构体化合物，其与3-乙酰氨基邻苯二甲酸酐经缩合反应得到目标化合物阿普斯特，其合成总产率相比传统合成方法提高了30%。阿普司特作为磷酸二酯酶-4(PDE-4)抑制剂，是一种口服药物，抑制参与银屑病发病机制中的多个炎症标志物的活性，可有效治疗银屑病。因此，本研究为其进一步工业化生产提供了理论基础。
이3-을양기-4-갑양기분정위원료제비득도1-(3-을양기-4-갑양기-분기)-2-갑광선기-을동，연후통과N-을선기L-량안산경화학탁분득도S형이구체화합물，기여3-을선안기린분이갑산항경축합반응득도목표화합물아보사특，기합성총산솔상비전통합성방법제고료30%。아보사특작위린산이지매-4(PDE-4)억제제，시일충구복약물，억제삼여은설병발병궤제중적다개염증표지물적활성，가유효치료은설병。인차，본연구위기진일보공업화생산제공료이론기출。
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.