A New Approach to Rapid Parallel Development of Four Neurokinin Antagonists. Part 4. Synthesis of ZD2249 Methoxy Sulfoxide

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• 作者：Sharon A. Bowden ; J. Nigel Burke ; Fiona Gray ; Steven McKown ; Jonathan D. Moseley ; William O. Moss ; Paul M. Murray ; Matthew J. Welham ; and Maureen J. Young
• 刊名：Organic Process Research & Development
• 出版年：2004
• 出版时间：January 2004
• 年：2004
• 卷：8
• 期：1
• 页码：33 - 44
• 全文大小：145K
• 年卷期：v.8,no.1(January 2004)
• ISSN：1520-586X

文摘

The manufacture of ZD2249 methoxy sulfoxide (1) using a newproject approach is described. Research department processeswere scaled up to 100 L if process safety and robustness werenot compromised; other factors were treated according to thenew approach. Using this strategy, we were able to manufacturea key intermediate on sufficient scale to support delivery of 1kg quantities of bulk drug within 6 months of the start of labwork.