Process Development and Scale-up of a Selective 1-Adrenoceptor Antagonist

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• 作者：Terrence J. Connolly ; Michael Matchett ; and Keshab Sarma
• 刊名：Organic Process Research & Development
• 出版年：2005
• 出版时间：January 2005
• 年：2005
• 卷：9
• 期：1
• 页码：80 - 87
• 全文大小：117K
• 年卷期：v.9,no.1(January 2005)
• ISSN：1520-586X

文摘

A synthetic route to a potent and selective -1-adrenergicreceptor antagonist has been developed and demonstrated in apilot plant. The route has been used in two pilot plantcampaigns and has produced RO3203546 in 2.3 and 12.0 kgbatch sizes. The first pilot plant campaign focused primarilyon the end-game of the process with particular emphasis onthe development of a method to isolate the active pharmaceutical ingredient (API). The second pilot plant campaign allowedfront-end process improvements to be demonstrated. Thereiterative process improvements resulted in an economicalprocess with improved throughput and product quality whencompared to the original discovery synthesis.