Dannhardt G, Kappe T, Meindl W, Schober B
Institut für Pharmazeutische Chemie der Johann Wolfgang Goethe-Universität Frankfurt.
Arch Pharm (Weinheim). 1990 Jun;323(6):375-9. doi: 10.1002/ardp.19903230610.
Reaction of ethyl 2-pyridyl acetates and activated malonates (magic malonates) leads to 1-ethoxycarbonyl-2-hydroxy-quinolizin-4-ones, which yield the corresponding C-1 unsubstituted derivatives by hydrolysis and decarboxylation. These compounds are catalytically hydrogenated to afford the corresponding tetrahydro derivatives. Significant inhibitory effects on mycobacterium tuberculosis H 37 Ra are shown, a structure-activity relationship is discussed.
2-吡啶基乙酸乙酯与活性丙二酸酯（神奇丙二酸酯）反应生成1-乙氧羰基-2-羟基喹嗪-4-酮，该产物通过水解和脱羧反应生成相应的C-1未取代衍生物。这些化合物经催化氢化得到相应的四氢衍生物。研究表明它们对结核分枝杆菌H 37 Ra具有显著的抑制作用，并讨论了构效关系。
