取代苯甲醛与取代2-羟基苯乙酮缩合形成α,β-不饱和酮(4a-4 f);4用H2O2氧化关环制得取代-3-羟基-2-取代苯基色酮(5a-5 f);5与2-氯-5-氯甲基吡啶反应合成了6个新型的含二氯五氯甲基吡啶结构的色酮类衍生物(6a-6 f),其结构经1H NMR,13C NMR和元素分析表征。初步体外活性实验结果表明,部分化合物具有较好的抗胃癌细胞(SGC-7901)活性。
α,β-Unsaturated ketones(4a~4f) were preparated by the condensation reaction of substituted benzaldehyde with substituted-2-hydroxyacetophenone.Six novel chromene derivatives(6a~6f) containing 2-chloro-5-chloromethylpyridine moiety were synthesized by the reaction of 2-chloro-5-chloromethylpyridine with substituted3-hydroxy-2-substituted-phenyl chromone(5a~5f),which were preparaed by the cyclization of 4 using H2O2 as the oxidant.The structures of 6 were caracterized by 1H NMR,13C NMR and elemental analysis.The preliminary in vitro assay tests showed that some compounds exhibited certain activity against human gastric cancer cell SGC-7901.