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Paper | Special issue | Vol 76, No. 1, 2008, pp. 715 - 726
Published online: 8th May, 2008
DOI: 10.3987/COM-08-S(N)68
Oxidative Conversion of Functionalized 3,4-Dihydopyrimidin-2(1H)-ones to the Corresponding Pyrimidin-2(1H)-ones Using Activated Carbon-Molecular Oxygen System

Ken-ichi Okunaga, Yukiko Nomura, Kenjiro Kawamura, Natsuki Nakamichi, Kazuo Eda, and Masahiko Hayashi*

*Department of Chemistry, Graduate School of Science, Kobe University, Nada, Kobe 657-8501, Japan

Abstract

Efficient synthesis of functionalized pyrimidin-2(1H)-ones was achieved by oxidation of 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) using activated carbon-molecular oxygen (O2) system. Various DHPMs were easily prepared by Biginelli reactions starting from aldehydes, β-ketoesters and urea. Therefore, the present method provides general and versatile protocol for the synthesis of a variety of functionalized pyrimidin-2(1H)-ones.

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