Implementation of a High-Temperature Claisen Approach for Early Phase Delivery of a Benzopyran Derivative

Control of trace inorganics and an understanding of reaction kinetics and impurity generation proved critical in allowing safe and reliable scale-up of a high-temperature Claisen reaction in support of multikilogram manufacture of a key chromene intermediate 4. Implementation of a Medicinal Chemistr...

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Bibliographic Details
Published in:	Organic process research & development Vol. 14; no. 1; pp. 85 - 91
Main Authors:	Walker, Andrew J, Adolph, Sven, Connell, Richard B, Laue, Klaus, Roeder, Michael, Rueggeberg, Carsten J, Hahn, Dirk Uwe, Voegtli, Kurt, Watson, John
Format:	Journal Article
Language:	English
Published:	American Chemical Society 15-01-2010
Online Access:	Get full text
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Summary:	Control of trace inorganics and an understanding of reaction kinetics and impurity generation proved critical in allowing safe and reliable scale-up of a high-temperature Claisen reaction in support of multikilogram manufacture of a key chromene intermediate 4. Implementation of a Medicinal Chemistry route allowed for rapid early phase delivery of 1 to support early clinical studies.
ISSN:	1083-6160 1520-586X
DOI:	10.1021/op900193v