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

Autor:	Sara Rossi, Paolo Stabile, Jason W. B. Cooke, Gilles Laval, Paola Russo, Roberta Pachera, Ramona Moretti, Pieter Westerduin, Zadeo Cimarosti, Nicola Giubellina, Francesco Tinazzi, William Maton
Rok vydání:	2011
Předmět:	Process development Computer science Genotoxic impurities Process research Organic Chemistry Pharmacology Combinatorial chemistry Quality by Design chemistry.chemical_compound chemistry medicine Anxiety Physical and Theoretical Chemistry medicine.symptom Derivative (chemistry)
Zdroj:	Organic Process Research & Development. 15:1287-1296
ISSN:	1520-586X 1083-6160
DOI:	10.1021/op200140v
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f192f5af1e4d746b5fb7e9edfa63ad2c https://doi.org/10.1021/op200140v Zobrazit plný text záznamu