Synthesis and reactivity of pyridylpyridone derivatives.
Synthesis and reactivity of pyridylpyridone derivatives.
复制标题
吡啶基吡啶酮衍生物的合成和反应性。
DOI：
10.1002/chin.200024140
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发表时间：
2000
期刊：
影响因子：
--
通讯作者：
N. Matsuo
中科院分区：
文献类型：
--
作者：
N. Sakamoto;Y. Kurita;K. Yanagi;N. Matsuo
众所周知，与母体化合物相比，将氟原子掺入生物活性分子中通常会导致活性增加。2，3-二氯-5-(三氟甲基)吡啶(1)是合成各种农药和医药的重要原料。1由1衍生的化合物具有很高的活性，部分归因于三氟甲基的存在。在我们不断寻找新的杀虫剂的研究中，我们合成了新的杀虫二聚体产品2。2化合物2通过与KF和KCN的亲核取代反应进行进一步的区域选择性修饰，分别得到了新的吡啶基吡啶酮3和4。
It is well-known that the incorporation of fluorine atoms into biologically active molecules often leads to increased activity compared to that of the parent compounds. 2, 3-Dichloro-5-(trifluoromethyl) pyridine (1) is an important starting material for various agrochemicals and pharmaceuticals. 1 The very high levels of activity of compounds derived from 1 can in part be attributed to the presence of the trifluoromethyl group. In our continuing research to find new insecticides, we synthesized the novel insecticidal dimeric product 2. 2 Further modification of compound 2 via nucleophilic substitution reactions with KF and KCN proceeded in a highly regioselective manner to afford the novel pyridylpyridones 3 and 4, respectively.