阿戈美拉汀的合成

Synthesis of Agomelatine

阿戈美拉汀由7-甲氧基四氢萘-1-酮与氰乙酸反应所得的(7-甲氧基-3,4-二氢-1-萘基)乙腈,经2,3-二氯-5,6-二氰基-1,4-苯醌芳构化制得(7-甲氧基-1-萘基)乙腈,再还原乙酰化"一锅"反应制得,总收率约76%。

Agomelatine was synthesized from 7-methoxytetralone and cyanoacetic acid by condensation and dehydrogenated by DDQ to give （7-methoxynaphthyl）acetonitrile which underwent one-step hydrogenation and acetylation in one pot with overall yield of 76 %.