论文部分内容阅读
以3-噻吩甲醛和氨基乙醛缩二甲醇为原料,经亲核加成、还原、取代、成环、甲酰化反应,得到2-醛基噻吩并[3,2-c]吡啶(4),然后与亚磷酸酯、芳香胺发生类Mannich反应得到一系列新型含有噻吩并[3,2-c]吡啶环的α-氨基膦酸酯类衍生物6a～6p.所有目标化合物的结构均经1H NMR,13C NMR,31P NMR,IR和MS确证.初步的生物活性测定试验表明,在50 ug/mL浓度下,大部分目标化合物对食管癌细胞(EC109)、人体肝癌细胞(HepG2)表现出较好的抑癌活性,其中化合物6k和6o对人体肝癌细胞的抑制率超过90%.
3-thiophenecarboxaldehyde and aminoacetaldehyde dimethyl acetal as raw materials, nucleophilic addition, reduction, substitution, cyclization, formylation reaction to give 2-aldehyde thieno [3,2-c] pyridine ) Followed by Mannich reaction with phosphite and aromatic amine to obtain a series of novel α-aminophosphonate derivatives 6a ~ 6p containing thieno [3,2-c] pyridine ring. All the structures of the target compounds The results of 1H NMR, 13C NMR, 31P NMR, IR and MS confirms that the preliminary bioassay results showed that most of the target compounds exhibited good performance on EC109 and HepG2 cells at the concentration of 50 ug / mL, A better anti-tumor activity, of which compound 6k and 6o on human liver cancer cells inhibition rate of more than 90%.