Synthesis of N-(1,3-dioxo-1,3-dihydrobenzofuran-4-yl)acetamide
N-(1,3-dioxo-l,3-dihydrobenzofuran-4-yl)acetamide,the key intermediate of Apremilast was prepared from 3-nitrophthalic acid via cyclization,reduction,and acetylation.The reaction conditions were optimized for the synthesis of N-(1,3-dioxo-1,3-dihydrobenzofuran-4-yl)acetamide.The total yield of the target compound was improved to 79.9％with the purity of 98.9％(HPLC),and the structure of target compound was identified by ESI-MS and 1H NMR.The improved process is facile and suitable for industrial production with relatively convenient operation procedures,and easily available raw material.
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