Development of an Efficient and Practical Route for the Multikilogram Manufacture of Ethyl 5-Cyano-2-methyl-6-oxo-1, 6-dihydropyridine-3-carboxylate and Ethyl 6- …

…, F Therkelsen, SM Andersen, F Zetterberg…

Index: Bell, Stephen J.; McIntyre, Steve; Garcia, Conchita F.; Kitson, Sean L; Therkelsen, Frans; Andersen, Soren M; Zetterberg, Fredrik; Aurell, Carl-Johan; Bollmark, Martin; Ehrl, Robert Organic Process Research and Development, 2012 , vol. 16, # 5 p. 819 - 823

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Abstract

Elucidation of the mechanism of formation of two major impurities in the synthetic route towards key intermediate ethyl 5-cyano-2-methyl-6-oxo-1, 6-dihydropyridine-3-carboxylate 1, led directly to the development of a route with significant process improvements in terms of yield, purity, and operability. The overall process yield increased from 15% to 73% without the need for extra purification steps, giving the key intermediate ethyl 6-chloro-5-cyano-2- ...