Synthesis of Tetramic Acid Derivatives via a Tandem Umpolung Alkylation/Reduction/Cyclization Reaction of γ-Hydrazono β-Ketoester.,Organic Letters

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Synthesis of Tetramic Acid Derivatives via a Tandem Umpolung Alkylation/Reduction/Cyclization Reaction of γ-Hydrazono β-Ketoester.
Organic Letters ( IF 4.9 ) Pub Date : 2020-03-31 , DOI: 10.1021/acs.orglett.0c00824
Isao Mizota ₁ , Miki Maeda ₁ , Kiho Imoto ₁ , Makoto Shimizu _{1,

2}

Affiliation

An efficient method for the one-pot synthesis of tetramic acid derivatives was developed utilizing tandem umpolung N-alkylation/reduction/cyclization of γ-hydrazono β-ketoester. By using this reaction as a key step, the total synthesis of the 3-spiro 7-hydroxamic acid tetralin which possesses an HDAC inhibitory activity was also achieved.

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