臺灣博碩士論文加值系統

近來, 合成一系列的 1, 6, 7, 8, 及 4'-取代-2-苯基-4-■■酮類
衍生物並檢視其細胞致毒活性。發現其中某些化合物具有細胞致毒活性。
因而, 在此研究中, 合成出 4-苯基-2-■■酮及一系列的 5-取代-2
-苯基-4-■■酮類化合物,並提出做細胞致毒活性的評估。
當苯胺和乙基‧甲苯醯基(代)乙酯縮合後, 在多磷酸中加熱至 140
∼150℃ 進行熱環化反應, 得到兩種異構產物：4-苯基-2-■■酮及 2-
苯基-4-■■酮。同樣地, 5,7-雙取代-2-苯基-4-■■酮及 5,8-雙取代-
2-苯基-4-■■酮分別由 3,5-雙取代苯胺及 2,5-雙取代苯胺所製備而得
。然而, 乙基‧甲苯醯胺(代)乙酯和間位取代(氟、甲基)苯胺經縮合而得
的中間產物, 再經熱環化後, 得到兩個異構產物：5-取代-2-苯基-4-■■
酮及7-取代-2-苯基-4-■■酮。
所合成出之化合物的篩選正在進行中, 容後再作報告。

Recently, a series of 1, 6, 7, 8, and 4'-substituted-2-
phenyl-4-quinolones were synthesized and examined for their
cytotoxicity. Some of these compounds were found to possess
significant cytotoxicity.
Therefore, in this study, 4-phenyl-2-quinolone and a series
of 5-substituted-2-phenyl-4-quinolone analogs were synthesized
and evaluated for their cytotoxicity.
When aniline was condensed wyth ethyl benzoylacetate
followedby a thermal cyclization in polyphosphoric acid at 140∼
150℃, two isomeric products：4-phenyl-2-quinolone and 2-phenyl
-4-quinolone were obtained. Similar, the 5,7-disubstituted-2-
phenyl-4-quinolones and 5,8-disubstituted-2-phenyl-4-quinolones
were prepared from the 3,5-disubstituted anilines and 2,5-disub-
stituted anilines, respectively. However, thermal cyclization of
the intermediated that obtained by acid condensation of ethyl
benzoylacetate with their corresponding m-substituted(fluoro,
methyl)aniline yielded two isomeric products：5-substituted-2-
phenyl-4-quinolone and 7-substituted-2-phenyl-4-quinolone.
The screening tests of the synthetic compounds are in
progress and will be reported later.