4-Pyrimidone-2-thioethers can be useful synthetic precursors to densely functionalized pyrimidines, commonly encountered in bioactive molecules. A convenient one-pot access to 4-pyrimidone-2-thioethers is reported herein, which utilizes a sequential base- and acid-mediated condensation of alkylisothioureas with β-ketoesters. Owing to mild reaction conditions, good to excellent functional group tolerance and yields are achieved. The utility of this approach is demonstrated by the synthesis of the crucial intermediate on a 200 gram scale.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10862098 | PMC |
| http://dx.doi.org/10.1039/d4ra00039k | DOI Listing |
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