Route Selection and Process Development for a 5-Piperazinylquinaldine Derivative for the Treatment of Depression and Anxiety

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• 作者：Zadeo Cimarosti ; Nicola Giubellina ; Paolo Stabile ; Gilles Laval ; Francesco Tinazzi ; William Maton ; Roberta Pachera ; Paola Russo ; Ramona Moretti ; Sara Rossi ; Jason W. B. Cooke ; Pieter Westerduin
• 刊名：Organic Process Research & Development
• 出版年：2011
• 出版时间：November 18, 2011
• 年：2011
• 卷：15
• 期：6
• 页码：1287-1296
• 全文大小：962K
• 年卷期：v.15,no.6(November 18, 2011)
• ISSN：1520-586X

文摘

1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone, 1, was identified as a potential drug for the treatment of depression and anxiety. Herein is described the work carried out to select the manufacturing route and the process research studies to optimize the key stages of route B. A particular focus is given to the genotoxic impurities, related to this route, as one of the intermediates of the manufacturing route was genotoxic and many genotoxic impurities can be formed in the process. Quality by Design principles were applied for the definition of the control strategy of these impurities.