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Condensation of substituted 2-aminopyridine with β-ketocarboxylic esters: 4H-pyrido[1,2-a]pyrimidin-4-ones and pyridin-2-ones

✍ Scribed by Pier Luigi Ferrarini; Claudio Mori; Clementina Manera; Filippo Mori; Vincenzo Calderone; Enrica Martinotti


Publisher
Journal of Heterocyclic Chemistry
Year
1999
Tongue
English
Weight
268 KB
Volume
36
Category
Article
ISSN
0022-152X

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✦ Synopsis


Abstract

We report the condensation of substituted 2‐aminopyridines 5 with β‐ketocarboxylic esters in polyphosphoric acid. In this reaction were obtained together with the target compounds, 4__H__‐pyrido[1,2‐a]pyrirnidin‐4‐ones 6 also the pyridin‐2‐ones 7. All the compounds 7 were tested for their calcium‐antagonistic activity but failed to evoke any vasorelaxant response.


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## Abstract magnified image The thienopyridine derivative **2**, obtained from reaction of acetoacetic ester with **1** in the presence of tin tetrachloride, was treated with triphenylphosphine in hexachloroethane and Et~3~N to give iminophosphorane **3**. Iminophosphorane **3** reacted with pheny