Identification of a Manufacturing Route of Novel CRF-1 Antagonists Containing a 2,3-Dihydro-1H-pyrrolo[2,3-b]pyridine Moiety

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• 作者：Arianna Ribecai ; Sergio Bacchi ; Monica Delpogetto ; Simone Guelfi ; Angelo Maria Manzo ; Alcide Perboni ; Paolo Stabile ; Pieter Westerduin ; Marie Hourdin ; Sara Rossi ; Stefano Provera ; Lucilla Turco
• 刊名：Organic Process Research & Development
• 出版年：2010
• 出版时间：July 16, 2010
• 年：2010
• 卷：14
• 期：4
• 页码：895-901
• 全文大小：343K
• 年卷期：v.14,no.4(July 16, 2010)
• ISSN：1520-586X

文摘

A case study on the synthesis of novel CRF-1 antagonists containing the 2,3-dihydro-1H-pyrrolo[2,3-b]pyridine moiety is presented. The development of ever more efficient synthetic routes allowed the progression of three candidates at the same time. A manufacturing route was identified and successfully demonstrated on a pilot-plant scale to prepare 100 kg of the CRF-1 antagonist GW876008.