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.
开发了一种高效的一锅法合成
四酸衍
生物的方法,该方法利用了串联反应中的γ-
肼基β-
酮酸酯的N-烷基化/还原/环化反应。通过将该反应用作关键步骤,还实现了具有H
DAC抑制活性的3-螺7-异羟
肟酸四氢
萘的全合成。