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

…, S Guelfi, AM Manzo, A Perboni, P Stabile…

Index: Ribecai, Arianna; Bacchi, Sergio; Delpogetto, Monica; Guelfi, Simone; Manzo, Angelo Maria; Perboni, Alcide; Stabile, Paolo; Westerduin, Pieter; Hourdin, Marie; Rossi, Sara; Provera, Stefano; Turco, Lucilla Organic Process Research and Development, 2010 , vol. 14, # 4 p. 895 - 901

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Citation Number: 10

Abstract

A case study on the synthesis of novel CRF-1 antagonists containing the 2, 3-dihydro-1 H- 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.