Synthesis of Novel Pyrido[1,2-α]pyrimidine-3-carboxamide Derivatives and Their Anticancer Activity
A series of novel pyrido[1,2-α]pyrimidine-3-carboxamide derivatives 6a-n were prepared starting from 2(1H) pyridone 1 via hydrolysis, de-carboxylation, selective ο-alkylation followed by rearrangement to give pyridine-2-amine 3. Compound 3 on reaction with ethoxy methylene malonic diethyl ester (EMM...
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Veröffentlicht in: | Chemical and Pharmaceutical Bulletin 2015-08, Vol.63 (8), p.584-590 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | jpn |
Online-Zugang: | Volltext |
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Zusammenfassung: | A series of novel pyrido[1,2-α]pyrimidine-3-carboxamide derivatives 6a-n were prepared starting from 2(1H) pyridone 1 via hydrolysis, de-carboxylation, selective ο-alkylation followed by rearrangement to give pyridine-2-amine 3. Compound 3 on reaction with ethoxy methylene malonic diethyl ester (EMME) under a conventional method followed by cyclization under micro wave irradiation (MWI) conditions resulted in product 5. Compound 5 on coupling with diverse substituted aliphatic amines formed title compounds 6a-n. All the products 6a-n were screened against four human cancer cell lines and compounds 6h-k and n which showed promising anticancer activity have been identified. |
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ISSN: | 0009-2363 |