The Development of an Effective Synthetic Route of Belinostat

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• 作者：Xuefei Bao ; Dake Song ; Xuejun Qiao ; Xuan Zhao ; Guoliang Chen
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：August 19, 2016
• 年：2016
• 卷：20
• 期：8
• 页码：1482-1488
• 全文大小：362K
• 年卷期：0
• ISSN：1520-586X

文摘

A practical synthetic route of belinostat is reported. Belinostat was obtained via a five-step process starting from benzaldehyde and including addition reaction with sodium bisulfite, sulfochlorination with chlorosulfonic acid, sulfonamidation with aniline, Knoevenagel condensation, and the final amidation with hydroxylamine. Key to the strategy is the preparation of 3-formylbenzenesulfonyl chloride using an economical and practical protocol. The main advantages of the route include inexpensive starting materials and acceptable overall yield. The scale-up experiment was carried out to provide 169 g of belinostat with 99.6% purity in 33% total yield.