Process Development and Scale-Up of an Hsp90 Inhibitor

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• 作者：Shengquan Duan ; Sripathy Venkatraman ; Xuechuan Hong ; Kenneth Huang ; Luckner Ulysse ; Bingidimi I. Mobele ; Alexander Smith ; Lawrence Lawless ; Andrew Locke ; Ravi Garigipati
• 刊名：Organic Process Research & Development
• 出版年：2012
• 出版时间：November 16, 2012
• 年：2012
• 卷：16
• 期：11
• 页码：1787-1793
• 全文大小：309K
• 年卷期：v.16,no.11(November 16, 2012)
• ISSN：1520-586X

文摘

A scalable process for the manufacture of a Hsp90 inhibitor was developed and optimized. Key features in the seven-step process include a selective S_NAr reaction followed by an Ullmann-type coupling of indazolone to an aryl halide. This improved process afforded 65% yield over two critical steps compared to 25% following the Medicinal Chemistry route.