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Efficient synthesis of highly functionalized tetrahydropyridopyrimidines by a novel three-component coupling reaction

✍ Scribed by Izzat T. Raheem; John D. Schreier; Michael J. Breslin

Publisher: Elsevier Science
Year: 2011
Tongue: French
Weight: 834 KB
Volume: 52
Category: Article
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2011.05.071

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✦ Synopsis

We report the development of a novel three-component coupling reaction (3CC) for the synthesis of alkoxy tetrahydropyridopyrimidines. Systematic optimization of reaction parameters identified 3CC conditions tolerant of a wide array of functionality at all three sites of diversity, providing densely functionalized products in moderate to excellent yields. The newly developed chemistry has since been applied to the lead optimization process on a novel drug discovery program, facilitating rapid compound advancement.

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